Antivascular and anticancer activity of dihalogenated A-ring analogues of combretastatin A-4?

MedChemComm Pub Date: 2010-08-23 DOI: 10.1039/C0MD00095G

Abstract

The generally accepted view is that the 3,4,5-trimethoxy-substituted aromatic A-ring of combretastatin A-4 (CA-4) and its analogues should be conserved in order to maintain biological activity through enforcing an active molecular conformation. Contrary to this, we have found that substituting the larger meta-methoxy groups of CA-4 with smaller halogen atoms results in compounds that are equipotent or more potent than CA-4 itself in vitro.

Graphical abstract: Antivascular and anticancer activity of dihalogenated A-ring analogues of combretastatin A-4
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