Design, synthesis and biological studies of novel tubulin inhibitors

  • Bioorg Med Chem Lett. 2013 Aug 1;23(15):4465-8. doi: 10.1016/j.bmcl.2013.04.078.
Yanjun Sun  1 ,  Bulbul Pandit ,  Somsundaram N Chettiar ,  Jonathan P Etter ,  Andrew Lewis ,  Jayasekar Johnsamuel ,  Pui-Kai Li
Affiliations
  • 1. 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.
PMID: 23790539 DOI: 10.1016/j.bmcl.2013.04.078
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.