Increased endothelial cell selectivity of triazole-bridged dihalogenated A-ring analogues of combretastatin A–1

…, PJ Bond, JD Brenton, DS Charnock-Jones…

Index: Beale, Thomas M.; Bond, Peter J.; Brenton, James D.; Charnock-Jones, D. Stephen; Ley, Steven V.; Myers, Rebecca M. Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 5 p. 1749 - 1759

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Citation Number: 13

Abstract

The antiproliferative activity on ovarian cancer (SK-OV-3) cells of a series of triazole-bridged combretastatin analogues (37, 38, 40–43) containing dihalogenation of the A-ring is reported, and compared with their trimethoxy analogues (5, 15, 39). It was found that dihalogenation with either bromine or iodine was a tolerated modification when compared to the parent compound combretastatin (CA–4, 1) and had less effect than B-ring ...