Anticancer properties of indole derivatives as IsoCombretastatin A-4 analogues
2021; Elsevier BV; Volume: 223; Linguagem: Inglês
10.1016/j.ejmech.2021.113656
ISSN1768-3254
AutoresShannon Pecnard, Abdallah Hamzé, Jérôme Bignon, Bastien Prost, Alain Deroussent, Laura Gallego‐Yerga, Rafael Peláez, Ji Yeon Paik, Marc Diederich, Mouâd Alami, Olivier Provot,
Tópico(s)Synthesis and biological activity
ResumoIn 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.
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