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Synthesis and development of New Bioactive Molecules. New therapeutic strategies

Publications and Patents


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. J. Med. Chem. 2017, 60 (4), pp 1523–1533.

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


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.


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.


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


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,

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


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.


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


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.


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 Tetrahedron 2009, 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.


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.