Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4

…, E Colomb, L Nachtergaele, S Thoret, J Dubois…

Index: Nguyen, Thi Thanh Binh; Lomberget, Thierry; Tran, Ngoc Chau; Colomb, Evelyne; Nachtergaele, Lore; Thoret, Sylviane; Dubois, Joelle; Guillaume, Joren; Abdayem, Rawad; Haftek, Marek; Barret, Roland Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 23 p. 7227 - 7231

Full Text: HTML

Citation Number: 13

Abstract

A novel series of combretastatin A-4 heterocyclic analogues was prepared by replacement of the B ring with indole, benzofurane or benzothiophene, attached at the C2 position. These compounds were evaluated for their abilities to inhibit tubulin assembly: derivative cis3b, having a benzothiophene, showed an activity similar to those of colchicine or deoxypodophyllotoxine. The antiproliferative and antimitotic properties of cis3b against ...