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ID: ALA1137780

Journal: J Med Chem

Title: Isocombretastatins a versus combretastatins a: the forgotten isoCA-4 isomer as a highly promising cytotoxic and antitubulin agent.

Authors: Messaoudi S, Tréguier B, Hamze A, Provot O, Peyrat JF, De Losada JR, Liu JM, Bignon J, Wdzieczak-Bakala J, Thoret S, Dubois J, Brion JD, Alami M.

Abstract: Herein is reported a convergent synthesis of isocombretastatins A, a novel class of potent antitubulin agents. These compounds having a 1,1-diarylethylene scaffold constitute the simplest isomers of natural Z-combretastatins A that are easy to synthesize without need to control the Z-olefin geometry. The discovery of isoCA-4 with biological activities comparable to that of CA-4 represents a major progress in this field.

CiteXplore: 19530698

DOI: 10.1021/jm900321u