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Accueil > Equipes de recherche > Chimie des ARN, nucléosides, peptides et hétérocycles > Thèmes de recherche

Chemistry of Heterocycles

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Insights into the interaction of high potency inhibitor IRC-083864 with phosphatase CDC25,
M. Sarkis, M.A. Miteva, M. Chiara Dasso Lang, M. Jaouen, M-A. Sari, M-O. Galcéra, M. Ethève-Quelquejeu, C. Garbay, G. Bertho, E. Braud, Insights into the interaction of high potency inhibitor IRC-083864 with phosphatase CDC25,
PROTEINS: Structure, Function, and Bioinformatics, 2017, 85, (4), 593–601.

Synthesis of novel 1,2,4-triazine scaffold as FAK inhibitors with antitumor activity,
P. Dao, D. Lietha, M. Etheve-Quelquejeu, C. Garbay, H. Chen,
Bioorg. Med. Chem. Lett., 2017, 27(8):1727-1730.

Routes of Synthesis of Carbapenems for Optimizing Both the Inactivation of l,d-Transpeptidase LdtMt1 of Mycobacterium tuberculosis and the Stability toward Hydrolysis by β-Lactamase BlaC
L. Iannazzo, D. Soroka, S. Triboulet, M. Fonvielle, F. Compain, V. Dubée, J.-L. Mainardi, J.-E. Hugonnet, E. Braud, M. Arthur*⊥, M. Etheve-Quelquejeu*
J. Med. Chem., 2016, 59 (7), 3427–3438

Synthesis of multifunctionalized 2-iminothiazolidin-4-ones and their 2-arylimino derivatives
Le Corre, L ; Dasso Lang, MC ; Garbay, C ; Gravier-Pelletier, C ; Busca, P ; Ethève-Quelquejeu, M ; Braud, E,
Synthesis, 2016, 2016; 48(24): 4569-4579.
Développement d'inhibiteurs des phosphatases CDC25 à potentialité anti-tumorale
Convenient Synthesis of 5-Arylidene-2-imino-4-thiazolidinone Derivatives Using Microwave Irradiation
M. Sarkis, D. N. Tran, M. C. Dasso Lang, C. Garbay, E. Braud*
Synlett 2014, 25, 1257-1262.


Kinetic features of L,D-transpeptidase inactivation critical for -lactam antibacterial activity”
S. Triboulet, V. Dubée, L. Lecoq, C. Bougault, J-L. Mainardi, L. B. Rice, M. Ethève-Quelquejeu, L. Gutmann, A. Marie, L. Dubost, J-E. Hugonnet, J-P. Simorre, M. Arthur,
PLOS ONE, 2013, 8, e67831.
Kinetic Analysis of Enterococcus faecium L,D-transpeptidase Inactivation by carbapenems
V. Dubée, M Arthur, H. Fief, S. Triboulet, J.-L. Mainardi, L. Gutmann, M. Sollogoub, L. B. Rice, M. Ethève-Quelquejeu, J-E. Hugonnet.
Antimicrob. Agents Chemother., 2012, 56, 3409-3412.
Inactivation of Mycobacterium tuberculosis L,D-transpeptidase LdtMt1 by carbapenems and cephalosporins.
V. Dubee, S. Triboulet, J-l. Mainardi, M. Ethève-Quelquejeu, L. Gutmann, A. Marie, L. Dubost, J-E. Hugonnet, M. Arthur,
Antimicrob. Agents Chemother., 2012, 56(8):4189.
Design and synthesis of novel bis-thiazolone derivatives as micromolar CDC25 phosphatase inhibitors: effect of dimerisation on phosphatase inhibition.
M. Sarkis, D.N. Tran, S. Kolb, M.A. Miteva, B.O. Villoutreix, C. Garbay, E. Braud*
Bioorg Med Chem Lett, 2012, 22, 7345-7350.

Rapid discovery of triazolobenzylidene-thiazolopyrimidines (TBTP) as CDC25 phosphatase inhibitors by parallel click chemistry and in situ screening.
R.A. Duval, S. Kolb, E. Braud, D. Genest, C. Garbay
J Comb Chem 2009, 11, 947-950.

Development of Novel Thiazolopyrimidines as CDC25B Phosphatase Inhibitors.
S. Kolb, O. Mondésert, M.L. Goddard, D. Jullien, B.O. Villoutreix, B. Ducommun, C. Garbay, E. Braud*
ChemMedChem 2009, 4 (4), 633-648.


Receptor-Based Virtual Ligand Screening for the Identification of Novel CDC25 Phosphatase Inhibitors.
M. Montes, E. Braud, M.A. Miteva, M.L. Goddard, O. Mondésert, S. Kolb, M.P. Brun, B. Ducommun, C. Garbay, B.O. Villoutreix
J Chem Inf Model 2008, 48, 157-165.