Synthesis and biological evaluation of vinylogous combretastatin A-4 derivatives

Organic & Biomolecular Chemistry Pub Date: 2005-06-21 DOI: 10.1039/B505955K

Abstract

Stereospecific syntheses of the ZE and EZ vinylogues of combretastatin A-4, and two B-ring related analogues, were achieved through a Suzuki–Miyaura coupling. As compared to CA4, the derivative with a phenyl moiety has shown increased potency in its ability to inhibit tubulin polymerisation.

Graphical abstract: Synthesis and biological evaluation of vinylogous combretastatin A-4 derivatives
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