Authors:
TM Beale, PJ Bond, JD Brenton, DS Charnock-Jones, SV Ley, RM Myers
Journal name: 
Bioorg Med Chem
Citation info: 
20(5):1749-1759
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 modification on potency. These compounds exhibited G(2)/M arrest, and maintained antitubulin activity. Further assays on human umbilical vein endothelial cells (HUVECs) demonstrated the potential antivascular effects of these triazoles. Of particular note was a 3,5-diiodo-4-methoxyaryl triazole (43) which had promising 7-fold selectivity for HUVECs over ovarian cancer cells.
DOI: 
http://doi.org/10.1016/j.bmc.2012.01.010
Research group: 
Brenton Group
E-pub date: 
01 Mar 2012