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A series of compounds originally derived from the vascular endothelial growth factor receptor tyrosine kinase inhibitor, SU5416, were synthesized and evaluated. The most potent compound in this series, compound 3, which structurally resembles the potent anti-microtubule agent combretastatin A-4, inhibited tubulin polymerization and showed potent growth inhibitory activities on both prostate and breast cancer lines with IC50 values in the low nanomolar range.

Original publication

DOI

10.1016/j.bmcl.2013.04.078

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

01/08/2013

Volume

23

Pages

4465 - 4468

Keywords

Antineoplastic Agents, Bibenzyls, Cell Line, Tumor, Cell Proliferation, Drug Design, Humans, Polymerization, Tubulin, Tubulin Modulators