Synthesis and development of New Bioactive Molecules. New therapeutic strategies

Synthesis and development of New Bioactive Molecules. New therapeutic strategies


The main objective of R. Benhida group over the last years has been to develop new chemical strategies to answer several challenging questions in biology and medicine using small organic molecules. This includes : the development of new synthetic methodologies, the development of modern drug discovery programs with the application of modern medicinal chemistry, nucleic acids chemistry and chemical biology for the identification and validation of new biological targets. The team has high contribution in the identification and validation of new bioactive molecules and novel relevant targets, particularly to overcome drug resistance in oncology.

 

Current fields of interest


  • Development of synthetic methodologies
  • ‘Smart’ Drug discovery : Medicinal Chemistry and Chemical biology
  • Nucleic acid chemistry

TEAM MEMBERS

 

 

Benhida Rachid (DR CNRS) - Team leader

Rachid.benhida@unice.fr

Rachid Benhida is DR CNRS, Deputy-Director of the ICN Institute and leader of Bioactive Molecules team. He received his Ph. D. from the University-Paris XI (1992). After three years postdoc         (Hoechst/Roussel-Uclaf, Germany and “Institut Curie-Paris”, 1994), he joined the “Institut de Chimie des Substances Naturelles” as “ANRS young research award” and as CNRS researcher in the same        year (1995). He moved to the University of Nice in 2002. His current researches focus on the development of synthetic methods and their applications in nucleic acid chemistry, chemical biology and the      development of new strategies to overcome drug resistance using small molecules (specific targeting of nucleic acids and CSCs, identification and validation of new targets, etc.)

 

 

 

 

Demange Luc (Pr.)

Luc.demange@unice.fr

 luc.demange@parisdescartes.fr

Luc Demange is a medicinal chemist, graduated from “Ecole Nationale Supérieure de Chimie de Paris”, who completed his PhD working on peptidyl-prolyl isomerases inhibitors (CEA/ Saclay, 2001). He was postdoctoral fellow in Sherbrooke (synthesis of cardiac glycosides) then in Montpellier (design of growth hormone secretagogues). In 2006, he was recruited as professor assistant (Paris Descartes University), and he developed with Prof. Christiane Garbay CDKs-inhibitors and Protein-Protein Interaction inhibitors, with potential applications in cancer treatment. He received in 2007 the "Award For Young Investigator in Medicinal Chemistry" (Institut de Recherches Servier) and he obtained his Habiliation to Manage Researches (HDR) in Pharmacochemistry in 2011.  
In 2013,LD moved to the “Institut de Chimie de Nice”, where his research interests are focused on the synthesis of new therapeutic agents to overcome drug resistances and to the development of new eco-compatible processes. In 2018 LD has been appointed as professor in organic chemistry at the Faculty of Pharmacy of Paris, and he moved to a new research unit, UMR 8036 CNRS “CiTCoM” in Paris. However, he continues to collaborate in depth with our team, in particular for the search of new anti-cancer drugs.
LD is deputy treasurer of the French Medicinal Chemistry Society (SCT, www.sct-asso.fr), in charge of the “Young Research Fellows Meeting”; he is also French delegate at the management committee of the European action COST-CA15135 MuTaLig, aiming at the identification of new chemical entities able to interfere concomitantly with various cellular targets (www.mutalig.eu).

 

 


Martin Anthony (CR CNRS)

Anthony.MARTIN2@univ-cotedazur.fr

Thématique de recherche:

- Conception et Synthèse d’agents anti-cancéreux principalement focalisés dans la lutte contre les hémopathies chimio-résistantes.

- Méthodologie de synthèse et Ingénierie d’acides nucléiques.

Anthony R. Martin received his PhD from the University of Montpellier in 2011 under the supervision of Prof. Michael Smietana and Dr. Jean-Jacques Vasseur, working on the synthesis and self-assembly of borono(oligo)nucleotides. He then joined Prof. Steven Nolan's group (Saint-Andrews University) as a postdoctoral researcher to work on late transition metal coordination and their applications in homogeneous catalysis. In 2013, he moved to the Institute of Chemistry of Nice in Dr. Benhida's group where he was appointed Chargé de Recherche— CNRS in 2014. His current researches focus on the design of new chemotherapeutics and encompass various aspects of nucleic acid chemistry.

 

 

Ronco Cyril (MC)

Ronco.Cyril@unice.fr

 

Cyril Ronco received his PhD on cholinesterases ligands under the supervision of Prof. P.-Y. Renard at the University of Rouen. He was then awarded with a Humboldt postdoctoral fellowship to work on the total synthesis of complex natural products in Prof. H.-D. Arndt group at Jena University, Germany. After working on medicinal chemistry projects in Prof. Déprez’s group (University of Lille), he joined in 2014 the group of Dr. Benhida as “Maître de Conférences” at the University of Nice Sophia Antipolis. His research focuses currently on the development of bioactive molecules to circumvent resistance mechanisms in the field of oncology.

 

 

 

 

Dao Pascal

Pascal.dao@unice.fr

Post-doctorant : Développement de nouveaux inhibiteurs de NIK pour potentialiser l’immunothérapie.

J’ai rejoint l’équipe Molécules Bioactives en 2016 en qualité de post-doctorant.

Après une formation de Biochimie et Biologie moléculaire à l’université Paris Diderot, je me suis dirigé vers la chimie du vivant avec un master en Chimie Médicinale et travailler sur le développement de nouveaux inhibiteurs de la protéine d’adhésion focale FAK à activité kinase dans le groupe du Pr. Christiane Garbay.

Pour mon 1er stage post-doctorale, j’ai rejoint l’équipe du Pr. Bernard Meunier à Guangzhou (Chine) pour travailler sur le développement de nouveaux outils diagnostiques de la maladie d’Alzheimer.

Je mets aujourd’hui à contribution mes compétences dans le développement et l’étude de nouveaux inhibiteurs de NIK, pour la potentialisation de l’immunothérapie.

 

 

Grytsai Oleksandr

Grytsai.oleksandr@unice.fr

3rd year PhD student (2015-2018) : "Development of new anticancer drugs to circumvent resistance mechanisms in oncology. Synthesis and biological application."

Oleksandr Grytsai received his B.S. in chemistry (2010) and M.S. (2012) in chemistry of natural products from Kyiv National Taras Shevchenko University.

In 2012 he was awarded a fellowship of the Ministry of Education and Science of Ukraine to perform a short internship at the Paul Sabatier University (Toulouse, France). The aim of the project was the synthesis of analogous of natural products and evaluation of their biological activity.

From 2012 to 2015 he undertook various positions as a research scientist and as a synthetic chemist at PBMR labs Ltd. (2012-2013), Curplyx Ltd. (2013-2014) and I.F. Lab Ltd. (2014-2015) where he was involved in design and synthesis of new biologically active molecules and small natural products.

At present, he is working toward his Ph.D. in organic and medicinal chemistry on discovery of new bioactive molecules with high therapeutic activity against various cancer cell lines at the Université Nice Côte d’Azur. His scientific interests include modern methods in organic synthesis, bioorganic and medicinal chemistry.

 

 

Safir-Fiho Mauro

Mauro.SAFIR-FILHO@unice.fr

ATER

 PhD degree in Chemistry from the Université Côte d’Azur, France, in 2018 (Molécules Bioactives group, under the supervision of Dr. Rachid Benhida and Dr. Anthony R. Martin). MS degree in Chemistry from the Universidade Federal do Rio Grande do Sul, Brazil (Federal University of Rio Grande Do Sul, UFRGS) in 2015 (Applied Organic Photochemistry research group, under the supervision of Prof. Fabiano Severo Rodembusch).

From the same university I got my bachelor’s degree in Industrial Chemistry in 2013 with honours (award for the outstanding academic performance). Currently, I have a one year position as “Attaché Temporaire d’Enseignement et de Recherche” (ATER) in the laboratory of Dr. Rachid Benhida at Université Côte d’Azur (Molécules Bioactives group). My research interests are in the fields of organic photochemistry and nucleic acid chemistry, with emphasis on the design of solvatochromic probes for biological applications and the development of novel methodologies applied to the post-synthetic functionalization of oligonucleotides.

  

 

Mateo Lou

Lou.mateo@univ-cotedazur.fr

PhD Student (2017-2020)



 

 

 

   

Fabre Marie

Marie.fabre@unice.fr

PhD Student (2018-2021)

Thesis : Design, synthesis and optimization of new cytokines receptors antagonists; Application to the treatment of AMD.

 

 

 

 

  

Talha Aicha

aicha.talha@etu.unice.fr

3rd year PhD Student (2017-2019): 

   -Development of new heterocyclic synthesis methodologies under ultrasound irradiations.

   -Development of a new anticancer family to circumvent the resistances in the hematologic tumors.

   Aicha Talha obtained her B.S. in organic chemistry (2013) and M.S. (2016) in organic and bioorganic chemistry from Mohammed V University of Rabat-Morocco. In 2016, she joined the team of plants chemistry and organic and bioorganic synthesis belonging to the research center: GEOPAC-MOROCCO as a PhD student of medicinal chemistry.

She joined the team of bioactive molecules in September 2018 for an internship of 10 months under the ERASMUS+ framework. And she was registered as an international PhD student at Côte d'Azur University where she is spending her 3rd year of PhD studies.
For the time being she puts her skills to work for the development of a new family of bioactive molecules analogues of Acadesine with high therapeutic activity to circumvent the resistances in the hematologic tumors.

 

Bardovskyi Rostyslav

Rostyslav.BARDOVSKYI@unice.fr

 PhD Student 

 

 

 

 

 

 

Dumond Aurore

dumond.aurore@gmail.com

 PhD Student (2018-2021) in Biology and Chemestry.

 

 

 

 

 

 

 

 

 

 

 

 

 

 

FORMER GROUP MEMBERS

 

 

DING Tianran

tianran.ding@cpe.fr

 

Etudiant Stagiaire M2.

Sujet : Développement de méthodologies de synthèse appliquées à la post-fonctionnalisation d'acides nucléiques.

 

 

 

 

 

 

 

 

 

 

 

 

Lagardère Prisca

plagardere@unice.fr

 

Etudiante stagiaire Master 2

Sujet : Synthèse de molécules anticancéreuses pharmacologiquement optimisées : 1,2,3-triazoles-1,4,5-trisubstitués.

 

 












Piroska Leonard

piroska_leonard@yahoo.com

 

Etudiant stagiaire en L3

Sujet : Synthèse d’une molécule ayant des effets anti-mélanome (HA 15) et de ses analogues. 













TCHUVAKOV Konstantin

Etudiant stagiaire en L2 chimie-biologie

Sujet : Synthèse de molécules anticancéreuses à partir de différentes guanidines et différents phényl isocyanate.

Purification, extraction, caractérisation. Modification structurale de certaines parties de la molécule afin d’optimiser l’activité de cette molécule sur la cible.

* Development of synthetic methodolgies

The central theme of our research is synthetic organic chemistry with a focus on the development of new synthetic methods based on various aspects of modern strategies including catalysis, tandem and multicomponent transformations, radical processes and their applications to the synthesis of biologically active molecules.


* ‘Smart’ Drug Discovery : Medicinal Chemistry and Chemical Biology

Developing new therapeutics for unmet medical needs and particularly in oncology continues to be an important focus of modern drug discovery. Our group is highly involved in the design, synthesis and validation of new ‘smart’ bioactive molecules featuring functional properties allowing them to interfere with several key biological processes including the metabolism, immune response and DNA damage checkpoint of cancer and cancer stem cells. Therefore, our drug discovery programs mainly focus on (i) the development of new smart small molecules to overcome drug resistance in oncology, through translational research with a closer integration, at an early stage, of chemistry/biology/clinic and industrial approaches ; and (ii) the identification & validation of new targets using chemical biology and “omics” approaches. To achieve this goal several collaborations have been established around the world with both academic and industrial partners.

o Targeting GRP78/Bip in cancer

Melanoma is an aggressive form of skin cancer that occurred in more than 230000 people and resulted in 55000 deaths in 2012, mainly in developed countries. Despite significant progress brought by the new anti-Braf and anti-PD1 targeted therapies, patients in the metastatic phase have a median life expectancy of only 8 - 9 months, because of the rapid emergence of resistance to these treatments. Thus it is of utmost importance to find new therapeutic approaches to treat these diseases.

GRP78 is a chaperone enzyme responsible for helping the proper folding of proteins synthesized in the ribosomes. It also acts as a molecular sensor of non-/misfolded protein accumulation, and triggers a cellular protection mechanism called UPR (Unfolded Protein Response) slowing down protein synthesis, and aiding the proper folding or the evacuation of these malformed proteins. Recently, we demonstrated, in collaboration with biologist partners from the Mediterranean Centre of Molecular Medicine (C3M) that the inhibition of GRP78 and UPR allowed circumventing these resistance phenomena by selectively inducing cell death in melanoma cells, without causing side effects or toxicity in non-cancerous cells. Therefore, we have developed new compounds inhibiting GRP78, active in vitro and in vivo, and displaying good pharmacological properties.

o Tackling the inflammation/angiogenesis axis in oncology

Inflammation and angiogenesis are two integrated processes. Our team develops series of small sized therapeutic agents able to interfere upstream and downstream of the corresponding signaling pathway.

  • New CXCL/CXCR antagonists : ongoing studies. We focused this project on the CXCL cytokine family because its leading member (IL-8) : (i) is abundantly secreted where and when VEGF is produced, (ii) its expression is comparable to these of VEGF, and (iii) the molecular factors of VEGF expression stimulate also IL-8 expression. As proof-of-concept, we already demonstrated that SB225002, a known competitive CXCR antagonist, inhibits tumor growth, angiogenesis and inflammation in vitro and in vivo in Clear Cell Renal Cell Carcinoma model (786-O cell line) by antagonizing the effect of CXCL 1, 7 and 8. We are currently working on the conception and the synthesis of new series of CXCR antagonists.
  • New Neuropilin antagonists. Neuropilin-1 (Nrp-1) is an VEGF-A co-receptor whose overexpression in tumor tissues is clinically related to a poor prognosis. We have developed the two first series of small-sized and non-peptidic Nrp-1 antagonists. The two lead compounds exert significant in vitro and in vivo anti-angiogenic and anti-tumor activities. We are currently working on : (i) deciphering the precise way-of-action of these lead compounds and (ii) optimizing their pharmacological profile.

 o Dual activation of autophagy and apoptosis to kill resistant cancer cells

Drug resistance is a major obstacle that limits the effectiveness of cancer therapy. Many cancer cells acquire resistance mechanisms that allow them to hamper apoptosis induction, contributing to initiation and progression of cancers. Therefore, novel therapeutic strategies are of great interest to address the emerging problem of drug resistance. Recent studies have suggested that the induction of autophagy, another type of cellular death mechanism different from apoptosis, could be a useful therapeutic approach to overcome drug resistance of cancers to some therapeutic agent, particularly those that typically induce an apoptotic response. Moreover, the existence of a complex functional relationship between apoptosis and autophagy can lead to cross-activation. Thus, the design of new chemotherapeutics able to induce simultaneously or consequently these two cell death types constitute an appealing approach to circumvent drug resistance. In this context we recently reported on novel nucleosides analogs able to revert the resistance to standard treatments in various haematological maligencies. For instance, we proved the efficacy of our nucleoside analogs, in vivo, on mice xenografted with the highly aggressive SKM1R cell line (myelodysplastic syndrome) whereas the first line treatment, azacitidine, is inefficient.

Ongoing studies concerning this dual targeting of apoptosis and autophagy are focused on (i) the understanding of the precise mode of action of our nucleoside analogs and (ii) the expansion of their application to non-hematological malignancies.

o Development of small molecules in cancer immunotherapy

Immune-checkpoint blockades are recent, major breakthroughs in cancer therapy but the response rate remains low (10% to 57% depending on the cancer type and the treatment combinations). While this approach relies on the use of large macromolecular structures (anti-bodies : anti-PD1, anti-PDL1) that “boost” the immune system, we are currently investigating the use of small synthetic organics able to potentiate both/either the immune system itself and/or the action of the anti-PD(L1). Our ongoing research in this field is mainly focused on the discovery of small therapeutics able to act synergistically with anti-PD1 antibodies (nivolumab, pembrolizumab).Immune-checkpoint blockades are recent, major breakthroughs in cancer therapy but the response rate remains low (10% to 57% depending on the cancer type and the treatment combinations). While this approach relies on the use of large macromolecular structures (anti-bodies : anti-PD1, anti-PDL1) that “boost” the immune system, we are currently investigating the use of small synthetic organics able to potentiate both/either the immune system itself and/or the action of the anti-PD(L1). Our ongoing research in this field is mainly focused on the discovery of small therapeutics able to act synergistically with anti-PD1 antibodies (nivolumab, pembrolizumab).

 * Nucleosides & Nucleic Acids Chemistry

 This part of research is focused on the chemistry and biochemistry of natural and artificial nucleosides and nucleic acids, with special emphasis on functional and structural properties of artificial short DNA and RNA. We also focus on the development of new synthetic methodologies using post-synthetic modifications with the aim of investigating functional key features of these important biomolecules in catalysis, labelling, cross-linking ... Biophysical properties and Biological activity of artificial nucleobases (DNA and RNA targeting, oligonucleotides and small molecule ligands), nucleosides, nucleotides and oligonucleotides is systematically studied in collaboration with several groups.

Multicomponent reactions

Rational design of DNA and RNA Ligands (Super-bases & supramolecular recognition)

Applications in DNAs targeting (artificial oligonucleotides TFO)

Applications in RNAs targeting




2018

  • Photoactivable DNA probes to trap single-stranded DNA binding proteins: updating the potential of 4-thiothymidine from a comparative study. T. Gérard-Hirne, F. Thiebaut, E. Sachon, A. Désert, T. Drujon, V.  Guérineau, B. Y. Michel, R. Benhida, S. Coulon, C. Saintomé and D. Guianvarc’h (2018). Biochimie 154, 164-175.
  • Building of neomycin-nucleobase-amino acid conjugates for the inhibition of oncogenic miRNAs biogenesis. D.D. Vo, C. Becquart, T.P.A. Tran, A. Di Giorgio, F. Darfeuille, C. Staedel, M. Duca (2018) Org Biomol. Chem., 16, 6262-6274.

  • A high-throughput screening of a chemical compound library in ovarian cancer stem cells. F. Ricci, L. Carrassa, M. S. Christodoulou, D. Passarella, B. Y. Michel, R. Benhida, N. Martinet, A. Hunyadi, E. Ioannou, V. Roussis, L. Musso, S. Dallavalle, R. Silvestri, N. Westwood, M. Mori, C. Ingallina, B. Botta, E. Kavetsou, A. Detsi, Z. Majer, F. Hudecz, S. Bősze, B. Kaminska, T.V. Hansen, P. Bertrand, C. M. Athanassopoulos, G. Damia (2018). Comb. Chem. High Throughput Screen, 21, 50-56.

  • Ultrasound-assisted facile one-pot sequential synthesis of novel sulfonamide-isoxazoles using cerium (IV) ammonium nitrate (CAN) as an efficient oxidant in aqueous medium. S. Alaoui, M. Driowya, L. Demange, R. Benhida, K. Bougrin (2018). Ultrason. Sonochem. 40, 289-297.

  • Identification of a new family of neuropilin-1 antagonists exerting anti-angiogenic and anti-tumour activities in vitro and in vivo. W.-Q. Liu, Y. Lepelletier, M. Montes, L. Borriello, B. Leforban, A. Loukaci, O. Hermine, S. Dufour, R. Benhida, C. Garbay, F. Raynaud, R. Hadj-Slimane, L. Demange (2018). Cancer Lett. 414, 88-98.

  • Design and Synthesis of Novel Styryl-Based Push-Pull Fluorophores. An Evaluation of the Structure-Photophysics Relationship. M. S. Filho, A. R. Martin, S. Fiorucci, R. Benhida (2018). New J. Chem. DOI: 10.1039/c7nj03142d 2018.

  • Modular synthesis of new C-aryl-nucleosides and their anti-CML activity. H. Marzag, M. Zerhouni, H. Tachallait, L. Demange, G. Robert, K. Bougrin, P. Auberger and R. Benhida (2018). Bioorg. Med. Chem. Lett, https://doi.org/10.1016/j.bmcl.2018.03.063.

  • Concise synthesis and antibacterial evaluation of novel 3-(1,4-disubstituted-1,2,3-triazolyl)uridine nucleosides. H. Tachallait, A. Bouyahya, A. Talha, Y. Bakri, N. Dakka, L. Demange, R. Benhida, K. Bougrin (2018). Arch Pharm Chem Life Sci. 1-11. DOI: 10.1002/ardp.201800204.

  • HA15, une nouvelle molécule qui pousse les cellules cancéreuses au suicide. C. Ronco, S. Rocchi, R. Benhida (2018). Actualité Chimique 429, 1-7.

2017

In Vitro and in Vivo Evaluation of Fully Substituted (5-(3-Ethoxy-3-oxopropynyl)-4-(ethoxycarbonyl)-1,2,3-triazolyl-glycosides as Original Nucleoside Analogues to Circumvent Resistance in Myeloid Malignancies.H. Amdouni, G. Robert, M. Driowya, N. Furstoss, C. Métier, A. Dubois, M. Dufies, M. Zerhouni, F. Orange, S. Lacas-Gervais, K. Bougrin, A. R. Martin, P. Auberger, R. Benhida. (2017J. Med. Chem., 60 (4), pp 1523–1533.

• Assessment of new triplet forming artificial nucleobases as RNA ligands directed towards HCV IRES IIId loop. M. Safir Filhoab, A.R. Martin and R. Benhida (2017). Bioorg. Med Chem. Lett. 1780-1783, http://dx.doi.org/10.1016/j.bmcl.2017.02.061.

Hypoxia Inducible Factor down-regulation, cancer and cancer stem cells (CSCs) : ongoing success stories. A.R. Martin, C. Ronco, L. Demange, R. Benhida. Med. Chem. Commun. 2017, 8, 295-319.

ATM, ATR, CHK1, CHK2 and WEE1 inhibitors in cancer and cancer stem cells. C. Ronco, A.R. Martin, L. Demange, R. Benhida. Med. Chem. Commun.2017, 8, 21-52.

Assessment of new triplet forming artificial nucleobases as RNA ligands directed towards HCV IRES IIId loop. M. Safir Filho, A. R. Martin, R. Benhida. Bioorg. Med. Chem. Lett. 2017. DOI. 10.1016/j.bmcl.2017.02.061

Targeting BIP to induce Endoplasmic Reticulum stress and cancer cell death. M. Cerezo, R. Benhida, S. Rocchi. Oncoscience 2017, DOI : 10.18632/oncoscience.

Synthesis and anti-cancer activities of new sulfonamides 4-substituted-1,2,3 triazolyl-nucleosides.S. Allaoui, M. Duffies, M. Driowya, L. Demange, K. Bougrin, G. Robert, P. Auberger, G. Pagès, R. Benhida. Bioorg. Med. Chem. Lett. 2017.

Asymmetric synthesis of glutamate derivatives. R. Seck, A. Gassama, M. Nour, L. Demange, C. Cavé. ARKIVOC 2017.

Metastatic Melanoma : Insights Into the Evolution of the Treatments and Future Challenges. A. Millet, A. R. Martin, C. Ronco, S. Rocchi, R. Benhida, Med. Res. Rev., 2017, 31, 98-148.

Structure activity relationship and optimization of N-(3-(2-aminothiazol-4-yl)aryl)benzenesulfonamides as anti-cancer compounds against sensitive and resistant cells. Cyril Ronco, Antoine Millet, Magali Plaisant, Patricia Abbe, Nedra Hamouda-Tekaya, Stéphane Rocchi and Rachid Benhida. Bioorg. Med. Chem. Lett. 2017. Just accepted

2016

Discovery and Optimization of N-(4-(3-Aminophenyl)thiazol-2-yl)acetamide as a Novel Scaffold Active against Sensitive and Resistant Cancer Cells. A. Millet, M. Plaisant, C. Ronco, M. Cerezo, P. Abbe, E. Jaune, E. Cavazza, S. Rocchi, R. Benhida. J. Med. Chem., 2016, 59 (18), pp 8276–8292.

Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance. M. Cerezo, A. Lehraiki, A. Millet, F. Rouaud, M. Plaisant, E. Jaune, T. Botton, C. Ronco, P. Abbe, H. Amdouni, T. Passeron, V. Hofman, B. Mograbi, A.-S. Dabert-Gay, D. Debayle, D.Alcor, N. Rabhi, J.-S. Annicotte, L. Héliot, M. Gonzalez-Pisfil, C. Robert, S. Moréra, A. Virougoux, P. Gual, M. M.U. Ali, C. Bertolotto, P. Hofman, R. Ballotti, R. Benhida, S. Rocchi. Cancer Cell, 2016, 29, pp 1-15. – Highlighted in Gr(i)p the ER to Stress Out Melanoma. W. Xu, L. Neckers. Cancer Cell Previews, 2016, 29, pp 769-770.

Microwave-assisted synthesis of bioactive seven-membered, macro-sized heterocycles and their fused derivatives. M. Driowya, A. Saber, H. Marzag, L. Demange, K. Bougrin, R. Benhida. Molecules. 2016, 21, 1032.

Microwave-assisted synthesis of bioactive six-membered heterocycles and their fused analogues.M. Driowya, A. Saber, H. Marzag, L. Demange, R. Benhida, K. Bougrin. 2016, 21, 492.

Solvent-free regioselective synthesis of novel isoxazoline and pyrazoline N-substituted saccharin derivatives under microwabe irradiation. A. Saber, M. Driowya, S. Alaoui, H. Marzag, L. Demange, E. Alvarez, R. Benhida, K. Bougrin. Chem. Heterocycl. Compd. 2016, 51, 31-40.

Biomimetic synthesis of urukthapelstatin A by Aza-Wittig ring contraction. S. Schwenk, C. Ronco, A. Oberheide, H.-D. Arndt. Eur. J. Org. Chem., 2016, pp 4795-4799.

On the Mechanism of the Digold(I) Hydoxide-Catalyzed Hydrophenoxyaltion of Alkynes. A. Gómez-Suárez, Y. Oonishi, A. R. Martin, S. V. C. Vummaleti, D. J. Nelson, D. B. Cordes, A. M. Z. Slawin, L. Cavallo, S. P. Nolan, A. Poater. Chem. Eur. J. 2016, 22, 1125-1132.

Scope and Limitations of the Dual-Gold-Catalysed Hydrophenoxylation of Alkynes. A. Gómez-Suárez, Y. Oonishi, A. R. Martin, S. P. Nolan Beilstein J. Org. Chem. 2016, 12, 172-178.

The Buchwald-Hartwig Reaction. A. R. Martin ; Book Chapter : N-Heterocyclic Carbenes in Catalytic Organic Synthesis Vol. 1. Science of Synthesis, 2016 (ISBN : 9783132012813) Ed. S. P. Nolan & C. S. J. Cazin.

Solvent-free regioselective synthesis of novel isoxazoline and pyrazoline N-substituted saccharin derivatives under microwave irradiation. A. Saber, M. Driowya, S. Alaoui, H. Marzag, L. Demange, E. Alvarez, R. Benhida, K. Bougrin. J. Het. Chem, 2016, 52, 31-40.

Dual emissive analogue of deoxyuridine as a sensitive hydration-reporting probe for discriminating mismatched from matched DNA and DNA/DNA from DNA/RNA duplexes. N. P. F. Barthes, K. Gavvala, D. Dziuba, D. Bonhomme, I. A. Karpenko, A. S. Dabert-Gay, D. Debayle, A. P. Demchenko, R. Benhida, B. Y. Michel, Y. Mély, A. Burger. J. Mater. Chem. C, 2016, 4, 3010-1017.

Oncogenic microRNAs biogenesis as a drug target : structure-activity relationship studies on novel aminoglycoside conjugates. D.D. Vo, T.P.A. Tran, C. Staedel, R. Benhida, A. Di Giorgio, M. Duca. Chem. Eur. J., 2016, 22, 5350-5362.

Novel Substituted Quilonine Compounds. R. Benhida, G. DeDonatis, A. R. Martin, T. Passeron. Patent, EP16305862.

2015

Disruption of phactr-1 pathway triggers pro-inflammatory and pro-atheriogenic factors : new insights at atherosclerosis development. R. Jarray, S. Pavoni, L. Borriello, B. Allain, N. Lopez, S. Bianco, W.-Q. Liu, D. Biard, L. Demange, O. Hermine, C. Garbay, F. Raynaud, Y. Lepelletier. Biochimie. 2015, 118, 151-161.

New peptides structurally-related to VEGF-A165 exon 7 and 8 encoded domains antagonize its binding to NRP-1 and VEGF-R1. W.-Q. Liu, L. Borriello, B. Allain, S. Pavoni, O. Hermine, C. Garbay, F. Raynaud, Y. Lepelletier, L. Demange. Int. J. Pept. Res. Ther. 2015, 21, 117-124.

Structure-activity relationships of imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human insulin-degrading enzyme. J. Charton, M. Gauriot, J. Totobenazara, N. Hennuyer, J. Dumont, D. Bosc, X. Marechal, J. Elbakali, A. Herledan, X. Wen, C. Ronco, H. Gras-Masse, A. Heninot, V. Pottiez, V. Landry, B. Staels, W.G. Liang, F. Leroux, W.-J. Tang, B. Deprez, R. Deprez-Poulain. Eur. J. Med. Chem., 2015, 90, pp 547-567.

Novel substituted hydrophobic benzenesulfonamide thiazole compounds. R. Benhida, S. Rocchi, C. Ronco, M. Plaisant, A. Millet, R. Balloti. European Patent 2015 EP15306213.8. International extension : PCT Int. Appl. 2017, WO2017017004A1.

"7,11-methanocycloocta[b]quinolone derivatives as Highly Functionalizable Acetylcholinesterase Inhibitors. C. Ronco, P.-Y. Renard, L. Jean, F. Nachon, A. Romieu. US Patent 2015, US9040506B2.

Composition and methods for the purification and production of butyrylcholinesterase. O. Lockridge, M.A. Larson, S.H. Schopfer, S.H. Hinrichs, F. Nachon, X. Brazolotto, C. Ronco, L. Jean, P.-Y. Renard, D. David. PCT Int. Appl. 2015, WO2015077317A1.

Efficient and Selective Azidation of per-O-Acetylated Sugars Using Ultrasound Activation : Application to the One-Pot Synthesis of 1,2,3-Triazole Glycosides. H. Marzag, S. Aloaoui, H. Amdouni, A. R. Martin, K. Bougrin, R. Benhida New J. Chem 2015, 39, 5437-5444.

Resistance to Sunitinib in Renal Clear Cell Carcinoma Results From Sequestration in Lysosomes and Inhibition of the Autophagic Flux. S. Giuliano, Y. Cormerais, M. Dufies, R. Grépin, P. Colosetti, A. Belaid, J. Parola, A. R. Martin, S. Lacas-Gervais, N. M. Mazure, R. Benhida, P. Auberger, B. Mograbi, G. Pagès Autophagy 2015, 11, 1891-1904.

Development of environmentally sensitive fluorescent and dual emissive deoxyuridine analogues.N. P. F. Barthes, I. A. Karpenko, D. Dziuba, M. Spadafora, J. Auffret, A. P. Demchenko, Y. Mély, R. Benhida, B. Y. Michel, A. Burger. RSC Advances, 2015, 5, 33536 – 33545.

DNA-Templated Borononucleic Acids Self Assembly : A Study of Minimal Complexity R. Barbeyron, A. R. Martin, J.-J. Vasseur, M. Smietana RSC Adv. 2015, 5, 105587-105591.

FeCl3-promoted and ultrasound-assisted synthesis of resveratrol O-derived glycoside analogs. H. Marzag, G. Robert, M. Dufies, K. Bougrin, P. Auberger, R. Benhida. Ultrason. Sonochem. 2015, 22, 15-21.

2014

Several human cyclin-dependent kinase inhibitors, structurally related to (R)-roscovitine, as new anti-malarial agents. S. Houzé, N.-T. Hoang, O. Lozach, J. LeBras, L. Meijer, H. Galons, L. Demange. Molecules. 2014, 19, 15237-15257.

Conformational analysis of polyconjugated protein-binding ligand by joint quantum chemistry and polarizable molecular mechanics. Adressing the issues of anisotropy, conjugation, polarization, and multipole transferability. E. Goldwaser, B. DeCourcy, L. Demange, C. Garbay, R. Raynaud, R. Hadj-Slimane, J.-P. Piquemal, N. Gresh. J. Mol. Model. 2014, 20, 1-24.

Reaction site-driven regioselective synthesis of AChE inhibitors. E. Oueis, G. Santoni, C. Ronco, O. Syzgantseva, V. Tognetti, L. Joubert, A. Romieu, M. Weik, L. Jean, C. Sabot, F. Nachon, P.-Y. Renard. Org. Biomol. Chem., 2014, 12, pp 156-161.

Synthesis and structure-activity relationship of non-peptidic antagonists of neuropilin-1 receptor.W.-Q. Liu, V. Megale, L. Borriello, B. Leforban, M. Montès, E. Goldwaser, N. GResh, J.-P. Piquemal, R. Hadj-Slimane, O. Hermine, C. Garbay, F. Raynaud, Y. Lepelletier, L. Demange. Bioorg. Med. Chem. Lett. 2014, 24, 4254-4259.

Structure-based discovery of a small non-peptidic neuropilins antagonist exerting in vitro and in vivo anti-tumor activity on breast cancer model. L. Borriello, M. Montès, Y. Lepelletier, B. Leforban, W.-Q. Liu, L. Demange, B. Delhomme, S. Pavoni, R. Jarray, J.-L. Boucher, S. Dufour, O. Hermine, C. Garbay, R. Hadj-Slimane, F. Raynaud. Cancer Lett. 2014, 349, 120-127.

Efficient C-N and C-S bond formation using the highly active [Ni(IPr*OMe)(allyl)Cl] pre-catalyst. A. R. Martin, D. J. Nelson, S. Meiries, A. M. Z. Slawin, S. P. Nolan Eur. J. Org. Chem. 2014, 2014, 3127-3131.

[Au]/[Pd] Multicatalytic Processes : Direct One-Pot Access to Benzo[c]chromenes and Benzo[b]furans. Y. Oonishi, A. Gómez-Suárez, A. R. Martin, A. M. Z. Slawin, S. P. Nolan Chem. Eur. J.2014, 42, 13507-13510.

Direct Synthesis of Partially Modified 2’-O-Pivaloyloxymethyl RNAs by a Base-Labile Protecting Group Strategy and Potential for Prodrug-Based Gene Silencing Applications. A. Biscans, M. Bos, A. R. Martin, N. Ader, G. Sczakiel, J.-J. Vasseur, C. Dupouy, F. Debart ChemBioChem 2014, 18, 2674-2679.

Rational design of a solvatochromic fluorescent uracil analogue with dual-band ratiometric response based on 3-hydroxychromone. D. Dziuba, I. A. Karpenko, N. P. F. Barthes, B. Y. Michel, A. S. Klymchenko, R. Benhida, A. P. Demchenko, Y. Mély, A. Burger. Chem. Eur. J. 2014, 20, 1998 – 2079.

Artificial nucleobase-amino acid conjugates : a new class of TAR RNA binding agents. J.P. Joly, G. Mata, P. Eldin, L. Briant, F. Fontaine-Vive, M. Duca, R. Benhida. Chem. Eur. J. 2014, 20, 2071 – 2079.

Natural polyphenols as inhibitors of DNA methyltransferases, H. Marzag, P. Warnault, N. Martinet K. Bougrin, R. Benhida. Book Chapter : In "Studies in Natural Products Chemistry". Atta-Ur-Rahman, (Ed), Elsevier, Amsterdam, Netherlands 2014, Chapter 7, vol. 41, 191-226

2013

Unified Azoline and Azole Syntheses by Optimized Aza-Wittig Chemistry. P. Loos, C. Ronco, M. Riedrich, H.-D. Arndt. Eur. J. Org. Chem., 2013, pp 3290-3315.

Crystal Structures of Human Cholinesterases in Complex with Huprine W and Tacrine : Elements of Specificity for Anti-Alzheimer’s Drugs Targeting Acetyl- and Butyrylcholinesterase. F. Nachon, E. Carletti, C. Ronco, M. Trovaslet, Y. Nicolet, L. Jean, P.-Y. Renard. Biochemical Journal, 2013, 453, pp 393-399.

Potent inhibitors of CDK5 derived from roscovitine : synthesis, biological evaluation and molecular modeling. L. Demange, F. Naït Abdellah, O. Lozach, Y. Frandin, N. Gresh, L. Meijer, H. Galons. Bioorg Med. Chem. Lett. 2013, 23, 125-131.

Synthesis and evaluation of new potent inhibitors of CK1 and CDK5 : two kinases involved in Alzheimer’s disease. L. Demange, O. Lozach, Y. Ferandin, N.-T. Hoang, L. Meijer, H. Galons. Med. Chem. Res. 2013, 22, 3247-3258.

The 1,2,4-triazole as a scaffold for the design of ghrelin receptor ligands : development of JMV 2959, a potent antagonist. A. Moulin, L. Brunel, D. Boeglin, L. Demange, J. Ryan, C. M’Kadmi, S. Denoyelle, J. Martinez, J.-A. Fehrentz. Amino Acids 2013, 44, 301-314.

Solvent-free aryl amination catalysed by [Pd-(NHC)] complexes. A. Chartoire, A. Boreux, A. R. Martin, S. P. Nolan, RSC Adv. 2013, 3, 3840-3843.

Boron and Nucleic acid chemistries : Merging the best of both worlds A. R. Martin, J.-J. Vasseur, M. Smietana, Chem. Soc. Rev. 2013, 42, 5684-5713 – Featured on the front cover of the issue.

Straightforward synthesis of [Au(NHC)X] (NHC = N-heterocyclic carbene, X = Cl, Br, I) complexes A. Collado, A. Gómez-Suárez, A. R. Martin, A. M. Z Slawin, S. P. Nolan, Chem. Commun. 2013, 49, 5541-5543.

Hydrophenoxylation of alkynes by cooperative gold catalysis Y. Oonishi, A. Gómez-Suárez, A. R. Martin, S. P. Nolan, Angew. Chem., Int. Ed. 2013, 52, 9767-9771.

Enhanced activity of [Ni(NHC)CpCl] complexes in arylamination catalysis A. R. Martin, Y. Makida, S. Meiries, A. M. Z. Slawin, S. P. Nolan, Organometallics 2013, 32, 6265-6270.

Recent Advances in Drug Design of Epidermal Growth Factor Receptor Inhibitors. P. Warnault, A. Yasri, M. Quivy, G. Chevé, C. Boriès, B. Fauvel, and R. Benhida*. Curr. Med. Chem. 2013, 20, 2043-2067.

Sono-Transition-Metal-Catalyzed One pot Three-step Synthesis of functionalized glycosyl-1,2,3-triazoles. M. Driowya, R. Benhida*, K. Bougrin*. Synth. Commun. 2013, 43, 1808-1817.

Targeting the Production of Oncogenic MicroRNAs with Multimodal Synthetic Small Molecules. D. Duy Vo, C. Staedel, L. Zehnacker, R. Benhida, F. Darfeuille, M. Duca. ACS Chem. Biol. 2013, dx.doi.org/10.1021/cb400668h.

Benzenesulfonamide Thiazole derivatives. Methods of preparation and biological applications. R. Benhida, S. Rocchi, M. Cerezo, M. Duca, R. Balloti. EP2013/073439.

2012

A sweet origin for the key congocidine precursor 4-acetamidopyrrole-2-carboxylate. S. Lautru, S. Lijiang, L. Demange, T. Lombès, H. Galons, G.L. Challis, J.-L. Pernodet. Angewandte Chem. 2012, 51, 7454-7458.

Human Butyrylcholinesterase produced in Insect Cells : Huprine-based Affinity Purification and Crystal Structure. X. Brazzolotto, M. Wandhammer, C. Ronco, M. Trovaslet, L. Jean, O. Lockridge, P.-Y. Renard, F. Nachon. FEBS Journal, 2012, 279, pp 2905-2916.

Screening of new Huprine Inhibitors of Acetylcholinesterases by Electrospray Ionization Ion Trap Mass Spectrometry. A. Ziemianin, C. Ronco, R. Dole, L. Jean, P.-Y. Renard, C.M. Lange. Journal of Pharmaceutical and Biomedical Analysis, 2012, 70, pp 1-5.

Huprine Derivatives as Sub-Nanomolar Human Acetylcholinesterase Inhibitors : From Rational Design to Validation by X-ray Crystallography. C. Ronco, E. Carletti, J.-P. Colletier, M. Weik, F. Nachon, L. Jean, P.-Y. Renard. Chem. Med. Chem., 2012, 7, pp 400-405. Selected as « V.I.P. Paper »

Dynamic boronic acid-mediated autoligation of DNA strands M. Smietana, A. R. Martin, J.-J. Vasseur, Pure Appl. Chem. 2012, 84, 1659-1667.

Borononucleotides as substrates/binders for human NMP kinases : Enzymatic and spectroscopic evaluation. C. El Amri, A. R. Martin, J.-J. Vasseur, M. Smietana, ChemBioChem 2012, 13, 1605-1612.

Extending the utility of [Pd(NHC)(cinnamyl)Cl] precatalysts : Direct arylation of heterocycles. A. R. Martin, A. Chartoire, A. M. Z. Slawin, S. P. Nolan, Beilstein J. Org. Chem., 2012, 8, 1637-1643.

The Oligonucleotides incorporating a 3-hydroxychromone as a fluorescent base surrogate a bicolor ratiometric fluorescent probe able to detect DNA – protein interactions. D. Dziuba, V. Y. Postupalenko, M. Spadafora, A. S. Klymchenko, V. Guérineau, Y. Mély, R. Benhida, A. Burger. J. Am. Chem. Soc. 2012, 34 (24), pp 10209–10213.

Small molecules DNA methyltransferases inhibitors. N. Martinet, B. Y. Michel, P. Bertrand and R. Benhida. Med. Chem. Commun. 2012, 3 (3), 263 – 273

Synthesis of new analogues of the alkaloid natural product Camalexin and their antitumor activitities. H. Marzag, L. Rivas, K. Bougrin, R. Benhida. Heterocycles 2012, 85, 1533-1535.

Sequence-specific base pair mimics are efficient topoisomerases IB inhibitors. P. Vekhoff, M. Duca, D. Guianvarch, R. Benhida, P. B. Arimondo. Biochemistry 2012 DOI : 10.1021/bi2012959

Microwave-assisted Sustainable Heterocyclic Chemistry. Three, four and five-membered rings. K. Bougrin, M. Driowya, R. Benhida, Book Chapter : In Targets in Heterocyclic Systems-Chemistry and Properties. Ed. O. A. Attanasi and D. Spinelli. ICS and Royal Chem. Soc Edition, 2012, Vol 15. pp 65-116.

Microwave-promoted green cycloaddition reactions. K. Bougrin, R. Benhida, Book Chapter : In Microwave in Organic Synthesis. Ed. A. De La Hoz and A. Loupy. Wiley-VCH, Third Ed 2012. pp 739-812.

Acadesine Derivatives, Products and Compositions including same, therapeutic uses thereof and methods for synthesizing same. 104. R. Benhida, P. Auberger, M. Driowya, A. Puissant, V. Malnuit. WO/2012/143624.

Nucleoside derivatives, methods of preparation and the composition comprising thereof. R. Benhida, A. Faraj, 2012/10650FR. Issued 2014.

2011

New Huprine Compounds Functionalized at Position 9 as Highly Potent Acetylcholinesterase Inhibitors. C. Ronco, R. Foucault, E. Gillon, P. Bohn, F. Nachon, L. Jean, P.-Y. Renard. Chem. Med. Chem., 2011, 6, pp 876-888.

Palladium-Catalyzed Preparation of N-Alkylated Tacrine and Huprine Compounds. C. Ronco, L. Jean, H. Outaabout, P.-Y. Renard. Eur. J. Org. Chem., 2011, 2, pp 302-310.

Labelled Huprine Derivatives and their use in Medical Imaging. C. Bouteiller, M. F. Mariani, C. Ronco, P.-Y. Renard, L. Jean, A. Romieu. European Patent 2010 EP10305372.4. International extension : PCT Int. Appl. 2011, WO2011124712A1.

Preparation of Huprine derivatives as Highly Functionalizable Acetylcholinesterase Inhibitors. C. Ronco, P.-Y. Renard, L. Jean, F. Nachon, A. Romieu. European Patent 2010 EP10305366.6. International extension : PCT Int. Appl. 2011, WO2011124713A1.

Regioselective synthesis of 3-carbo-5-phosphonylpyrazoles through a one-pot Claisen-Schmidt/1,3-dipolar cycloaddition/oxidation sequence. A. R. Martin, K. Mohanan, L. Toupet, J.-J. Vasseur, M. Smietana, Eur. J. Org. Chem. 2011, 2011, 3184-3190.

Dynamic and programmable DNA-templated boronic ester formation. A. R. Martin, I. Barvik, D. Luvino, M. Smietana, J.-J. Vasseur, Angew. Chem., Int. Ed. 2011, 50, 4193-4196.

A mild and efficient protocol for the protection of 3-hydroxychromones under phase-transfer catalysis. D. Dziuba, R. Benhida, A. Burger. Synthesis 2011, 13, 2159-2164.

Targeting DNA base pair mismatch with artificial nucleobases. Recent advances and perspectives in triple helix strategy. M. Duca, V. Malnuit, R. Benhida. Org. Biomol. Chem. 2011, 9, 326-336.

Recent advances in microwave-assisted heterocyclic chemistry. Synthesis of three, four and five-membred heterocycles, M. Driowya, K. Bougrin, R. Benhida, Book Chapter : in “Targets in Heterocyclic Systems-Chemistry and Properties”, O.A. Attanasi and D. Spinelli (Eds), ICS&RCS, Vol.15, 2011, pp. 327-371

2010

A Fluorescent Immunochromatographic Test using Immunoliposomes for Detecting Microcystins and Nodularins. N. Khreich, P. Lamourette, B. Lagoutte, C. Ronco, X. Franck, C. Créminon, H. Volland. Anal. Bio. Chem., 2010, 397, pp 1733-1742.

Facile and Rapid Access to Linear and Truncated Microcystin Analogues for the Implementation of Immunoassays. G. Clavé, C. Ronco, H. Boutal, N. Khreich, H. Volland, X. Franck, A. Romieu, P.-Y. Renard. Org. Biomol. Chem., 2010, 8, pp 676-690. - Selected as « Hot Article 2010 »

Preparation of perharidines as CDK inhibitors. K. Bettayeb, N. Oumata, L. Demange, L. Meijer, H. Galons. Patent. US 20100280065.

Three-component reaction using the Bestmann-Ohira reagent : a regioselective synthesis of phosphonyl pyrazole rings. K. Mohanan, A. R. Martin, L. Toupet, M. Smietana, J.-J. Vasseur, Angew. Chem., Int. Ed. 2010, 49, 3196-3199.

Microwave assisted an efficient solvent-free Knoevenagel condensation. A sustainable protocol using porous calcium hydroxyapatite as catalyst. S. Mallouk, K. Bougrin, A. Laghzizil, R. Benhida. Molecules 2010, 15, 813-823.

Design of novel RNA ligands that bind to HIV-1 TAR RNA. Maria Duca, Vincent Malnuit, Florent Barbault, R. Benhida. Chem Comm 2010, 46, 6162-6164.

2009

Synthesis and Structure Activity Relationship of Huprines Derivatives as Human Acetylcholinesterase Inhibitors. C. Ronco, G. Sorin, F. Nachon, R. Foucault, L. Jean, A. Romieu, P.-Y. Renard. Bioorg. Med. Chem., 2009, 17, pp 4523–4536.

Anorexigenic and electrophysiological actions of novel ghrelin receptor (GHS-R1A) antagonists in rats. N. Salomé, D. Haage, D. Perrissoud, A. Moulin, L. Demange, E. Egecioglu, J.-A. Fehrentz, S.L. Dickinson. Eur. J. Pharmacol. 2009, 612, 167-173.

Perharidines as CDK inhibitors in the treatment of proliferative diseases. Patent. WO2009034475 & WO2009034411

Assessment of new 2’-O-acetalester protecting groups for regular and original 2’-modified proRNA.A. R. Martin, T. Lavergne, J.-J. Vasseur, F. Debart, Bioorg. Med. Chem. Lett. 2009, 19, 4046-4049.

Expanding the borononucleotide family : synthesis of the borono-analogues of dCMP, dGMP and dAMP. A. R. Martin, K. Mohanan, D. Luvino, N. Floquet, C. Baraguey, M. Smietana, J.-J. Vasseur, Org. Biomol. Chem. 2009, 7, 4369-4377 – Selected as a “Hot Paper” and featured on the cover of the issue.

From intriguing reactivity of 2-bromothiophene to the first synthesis of C1’-disubstituted C-nucleosides. C. Peyron and R. Benhida Synlett 2009, 3, 472-476.

Efficient Synthesis of Ratiometric Fluorescent Nucleosides Featuring 3-Hydroxy-Chromone nucleobases. M. Spadafora, V. Postopalenko, A. Klemchenko, Y. Mély, A. Burger, R. Benhida Tetrahedron2009, 65, 7809-7816.

Tandem Azide-Alkyne 1,3-Dipolar Cycloaddition-halogenation. A Concise one pot three component route to 4,5-di-substitued Triazolyl-Nucleosides. V. Malnuit, M. Duca, A. Manout, K. Bougrin, R. Benhida. Synlett 2009, 13, 2123-2128.

Synthesis and Structure of 1-(3-p-tolylisoxazol-5-yl)-Cyclohexanol. W. Khalil, K. Bougrin, R. Benhida, M. Soufiaoui, L. ElAmmari Acta Cryst. 2009. 2971-2973.

Tandem Azide-Alkyne 1,3-Dipolar Cycloaddition-halogenation. A Concise one pot three component route to 4,5-di-substitued Triazolyl-Nucleosides. V. Malnuit, M. Duca, A. Manout, K. Bougrin, R. Benhida. Synlett 2009, 13, 2123-2128.

Efficient synthesis of a- and b-2’-deoxy-heteroaryl-C-nucleosides. M. Spadafora, A. Burger, R. Benhida. Synlett 2009, 8, 1225-1229.

2008

Roscovitine-derived, dual specificity inhibitors of cyclin-dependent kinases (CDKs) and casein kinase 1 (CK1). N. Oumata, K. Bettayeb, Y. Ferandin, L. Demange, A. Lopez-Giral, M.-L. Goddard, V. Myrianthopoulos, E. Mikos, M. Flajolet, P. Greengard, L. Meijer, H. Galons. J. Med. Chem. 2008, 51, 5229-5242.

Synthesis of 6-pyridylaminopurines. L. Demange, N. Oumata, J. Quinton, S. Bouaziz, O. Lozach, L. Meijer, H. Galons. Heterocycles 2008, 74, 1735-1743.

New trisubstituted 1,2,4-triazole derivatives as potent GHS-R1a Antagonists. Synthesis and pharmacological in vitro and in vivo evaluations. A. Moulin, L. Demange, J. Ryan, D. Mousseaux, A. Heitz, G. Bergé, D. Gagne, D. Perrissoud, V. Locatelli, A. Torsello, J.-C. Galleyrand, J.-A. Fehrentz, J. Martinez J. Med. Chem. 2008, 51, 689-693.

Trisubstituted 1,2,4-triazoles as ligands for the ghrelin receptor : on the significance of the orientation and substitution at position 3. A. Moulin, L ; Demange, J. Ryan, C. M’Kadmi, J.-C. Galleyrand, J. Martinez, J.-A. Fehrentz. Bioorg Med. Chem. Lett. 2008, 18, 164-168.

Efficient synthesis of a- and b-2’-deoxy-heteroaryl-C-nucleosides. M. Spadafora, A. Burger*, R. Benhida Synlett 2008, 8, 1225-1229.

A Modified Friedel-Craft-Vorbrugen Reaction. Expetidious Two Steps Synthesis of Aryl and Heteroaryl C-Nucleosides. M. Spadafora, M. Mehiri, A. Burger, R. Benhida Tetrahedron Lett 2008, 49, 3967-3971.

Efficient synthesis and in vitro cytostatic activity of 4-substitued triazolyl-nucleosides. K. El Akri, K. Bougrin, J. Balzarini, A. Faraj, R. Benhida. Bioorg. Med. Chem. Lett. 2008, 17, 6656-6659.

A Stereo- and Regio-Controlled Synthesis of Bromothiophenyl-C-Nucleosides. Tandem Bromination-Glycosydation via Halogen Dance Process. C. Peyron, J.M. Navarre, D. Dubreuil, P. Vierling, R. Benhida Tetrahedron Lett. 2008, 49, 6171-6174.

What's next ?

June 2019

Cyril RONCO will present "Nouvelles approches pour contrer les mécanismes de résistance en oncologie. Synthèse, méthodologie et applications biologiques" the 25th of June in order to obtain his HDR.

What happened ?

February 2019

Anthony MARTIN obtained his HDR entitled : "De la catalyse et la chimie médicinale à l'ingénierie d'acides nucléiques artificiels.".

December 2018

Oleksandr Grytsai defended his PhD : "Design, synthesis and development of new biguanide-like molecules to circumvent drug resistance in melanoma.".

November 2018

Mauro Safir-Fiho defended his PhD : "Nucleic Acid Ligands and Benzothiazole-Based Fluorophores. Synthesis and Biological Applications.".

en cours de rédaction


en cours de rédaction


Rachid Benhida

  • Université Nice Sophia Antipolis, 
    U.F.R Sciences, 
    Institut de Chimie de Nice, UMR CNRS 7272, 
    28 avenue de Valrose, 
    06108 Nice, Cedex 2, 
    France
  • Rachid.BENHIDA@unice.fr
  • +33492076143 
    +33492076189

  

Team RB (2017)

26ème journée de la Chimie (Société Chimique de France, Section PACA)

Poster session, oral communication, sensoriel test. 

     

   

3rd WG meeting of COST MuTaLig. (CA15135) Fev.2019

Oral communication of Lou MATEO (Award by GENOCHEM): Synthesis and antagonist study of CXCR1 and CXCR2 receptors for oncology applications.

 

26th Young Research Fellow Meeting (YRFM-JJC Fev. 2019) in Paris.

Oral communication of Pascal DAO : Development of highly sensitive fluorescent probes for the real-time monitoring of senescence in live cells.

 

Oral communication of Aurore DUMOND : Opposite effect of NRP-1 and NRP-2 in the agressiveness of clear cell Renal Cell Carcinoma.

 

Oral communication of Cyril RONCO (SCT Award for young investigators in medicinal chemistry) : ER stress inducers targeting resistant cancers.

  

Flash poster presentation of Aicha TALHA : 

   

Memories of the congres.

        

HDR MARTIN Anthony (Février 2019)


 

Team RB (2017)