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Anticancer Properties of Indole Derivatives as IsoCombretastatin A-4 analogues

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Pecnard, Shannon | Hamze, Abdallah | Bignon, Jérome | Prost, Bastien | Deroussent, Alain | Gallego-Yerga, Laura | Peláez, Rafael | Paik, Ji Yeon | Diederich, Marc | Alami, Mouâd | Provot, Olivier

Edité par CCSD ; Elsevier -

International audience. 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 Bring separated by a N-methyl linker displayed a remarkable subnanomolar level of cytotoxicity (IC 50 < 1 nM) against 9 human cancer cell lines.

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