A-ring dihalogenation increases the cellular activity of combretastatin-templated tetrazoles

…, JD Brenton, DS Charnock-Jones, SV Ley…

Index: Beale, Thomas M.; Allwood, Daniel M.; Bender, Andreas; Bond, Peter J.; Brenton, James D.; Charnock-Jones, D. Stephen; Ley, Steven V.; Myers, Rebecca M.; Shearman, James W.; Temple, Jill; Unger, Jessica; Watts, Ciorsdaidh A.; Xian, Jian ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 3 p. 177 - 181

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Citation Number: 11

Abstract

The combretastatins have been investigated for their antimitotic and antivascular properties, and it is widely postulated that a 3, 4, 5-trimethoxyaryl A-ring is essential to maintain potent activity. We have synthesized new tetrazole analogues (32–34), demonstrating that 3, 5- dihalogenation can consistently increase potency by up to 5-fold when compared to the equivalent trimethoxy compound on human umbilical vein endothelial cells (HUVECs) ...