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A series of compounds originally derived from the vascular endothelial growth factor receptor tyrosine kinase inhibitor, SU5416, was synthesized and evaluated. The most potent compound in this series, compound 7, 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 IC(50) values in low to subnanomolar range.

Original publication

DOI

10.1016/j.bmcl.2005.09.001

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

15/12/2005

Volume

15

Pages

5382 - 5385

Keywords

Animals, Antineoplastic Agents, Brain, Cell Division, Indoles, Models, Molecular, Molecular Conformation, Pyrroles, Stilbenes, Swine, Tubulin