From a drug repositioning to a structure-based drug design approach to tackle acute lymphoblastic leukemia

Autor: Magali Saez-Ayala, Laurent Hoffer, Sébastien Abel, Khaoula Ben Yaala, Benoit Sicard, Guillaume P. Andrieu, Mehdi Latiri, Emma K. Davison, Marco A. Ciufolini, Paul Brémond, Etienne Rebuffet, Philippe Roche, Carine Derviaux, Edwige Voisset, Camille Montersino, Remy Castellano, Yves Collette, Vahid Asnafi, Stéphane Betzi, Patrice Dubreuil, Sébastien Combes, Xavier Morelli

Publikováno v: Nature Communications, Vol 14, Iss 1, Pp 1-17 (2023)

Abstract Cancer cells utilize the main de novo pathway and the alternative salvage pathway for deoxyribonucleotide biosynthesis to achieve adequate nucleotide pools. Deoxycytidine kinase is the rate-limiting enzyme of the salvage pathway and it has r

Externí odkaz: https://doaj.org/article/455ce64ed58b44c582373ae5edcfa6e5

Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins

Autor: Carine Derviaux, Stefan Knapp, Yuliia V. Voitovich, Brigitt Raux, Stéphane Priet, Jean Michel Brunel, Yves Collette, Sabine Milhas, Stephane Betzi, Eric Trinquet, Alexey Yu. Fedorov, Philippe Roche, Thomas Roux, Etienne Rebuffet, Adrien Lugari, Sebastien Combes, Jean-Claude Guillemot, Xavier Morelli

Publikováno v: Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, American Chemical Society, 2016, 59 (4, SI), pp.1634-1641. ⟨10.1021/acs.jmedchem.5b01708⟩
Journal of Medicinal Chemistry, 2016, 59 (4, SI), pp.1634-1641. ⟨10.1021/acs.jmedchem.5b01708⟩

A midthroughput screening follow-up program targeting the first bromodomain of the human BRD4 protein, BRD4(BD1), identified an acetylated-mimic xanthine derivative inhibitor. This compound binds with an affinity in the low micromolar range yet exert

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c7590b387ffd91787b0c43c63c187825
https://hal.archives-ouvertes.fr/hal-01439086

Synthesis of hydrophilic and lipophilic 4-arylcoumarin phosphates

Autor: Alexander V. Nyuchev, Yulia B. Malysheva, A. Yu. Fedorov, Sebastien Combes, Nikolay S. Sitnikov, A. N. Selikhov, Andrey S. Shavyrin, E. A. Sharonova

Publikováno v: Russian Chemical Bulletin. 60:2003-2009

Novel hydrophilic and lipophilic prodrugs, sodium 4-arylcoumarin dialkylphosphates and 4-arylcoumarin dioleyl phosphates, were synthesized by phosphorylation of 4-arylcoumarins with dialkylphosphites.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0855305eb0274dfa7f763e4a96a745bc
https://doi.org/10.1007/s11172-011-0304-7

On the optical activity of the 3-aryl-4-hydroxycoumarin isolated from Millettia griffoniana: molecular modelling and total synthesis

Autor: Didier Siri, Jean-Pierre Finet, Sebastien Combes

Publikováno v: Journal of the Chemical Society, Perkin Transactions 1. :38-44

Semi-empirical calculations on 4-hydroxy-3-(3′,4′-methylenedioxyphenyl)-5,6,7-trimethoxycoumarin, a natural product recently isolated from Millettia griffoniana, show low rotational barriers for the C(3)–C(1′) bond (19.9 kJ mol−1) and for t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::646569ad22ecff692f3710edb9d20d59
https://doi.org/10.1039/b108707j

Influence of the steric hindrance of the aryl group of pentavalent triarylbismuth derivatives in ligand coupling reactions

Autor: Jean-Pierre Finet, Sebastien Combes, Alexey Yu. Fedorov

Publikováno v: Tetrahedron. 55:1341-1352

Tris(ortho-tolyl)bismuth dichloride derivatives react with nucleophiles under basic conditions to give good to high yields of the C-arylated substrates. Under the same conditions, trimesitylbismuth dichloride affords only poor yields of the C-mesityl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0e481d113f45557100d324d5c6322cce
https://doi.org/10.1016/s0040-4020(98)01185-5