Authors
Shannon Pecnard, Abdallah Hamze, Jérome Bignon, Bastien Prost, Alain Deroussent, Laura Gallego-Yerga, Rafael Peláez, Ji Yeon Paik, Marc Diederich, Mouad Alami, Olivier Provot
Publication date
2021/11/5
Journal
European Journal of Medicinal Chemistry
Volume
223
Pages
113656
Publisher
Elsevier Masson
Description
In this study, a variety of original ligands related to Combretastatin A-4 and isoCombretastatin A-4, able to inhibit the tubulin polymerization into microtubules, was designed, synthesized, and evaluated. Our lead compound 15d having a quinazoline as A-ring and a 2-substituted indole as B-ring separated by a N-methyl linker displayed a remarkable sub-nanomolar level of cytotoxicity (IC50 < 1 nM) against 9 human cancer cell lines.
Total citations
202120222023202426107
Scholar articles
S Pecnard, A Hamze, J Bignon, B Prost, A Deroussent… - European Journal of Medicinal Chemistry, 2021