Design, synthesis and biological studies of novel tubulin inhibitors.

Bioorg Med Chem Lett

Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 338 Parks Hall, 500 West 12th Avenue, Columbus, OH 43210-1291, United States.

Published: August 2013

AI Article Synopsis

  • A series of compounds were developed from the inhibitor SU5416, focusing on their potential anti-cancer properties.
  • The most effective compound, identified as compound 3, shares structural similarities with the anti-cancer agent combretastatin A-4.
  • Compound 3 strongly inhibited tubulin polymerization and effectively suppressed the growth of prostate and breast cancer cells, showcasing low nanomolar IC50 values.

Article Abstract

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.

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Source
http://dx.doi.org/10.1016/j.bmcl.2013.04.078DOI Listing

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