Antimitotic activity of structurally simplified biaryl analogs of the anticancer agents colchicine and combretastatin A4

  • Bioorg Med Chem Lett. 2015 Jan 1;25(1):117-21. doi: 10.1016/j.bmcl.2014.10.090.
James McNulty  1 ,  Sean van den Berg ,  Dennis Ma ,  Daniel Tarade ,  Seema Joshi ,  Julia Church
Affiliations
  • 1. Department of Chemistry and Chemical Biology, McMaster University, 1280 Main Street West, Hamilton, Ont. L8S 4M1, Canada.
PMID: 25466200 DOI: 10.1016/j.bmcl.2014.10.090
Abstract

Two substituted biaryl analogues of colchicine and combretastatin A4, readily available through a one-step, protecting group free Suzuki-Miyaura reaction were discovered to exhibit Anticancer activity while simultaneously being of low cytotoxicity to noncancerous cell lines. The compounds were shown to initiate Apoptosis selectively via a mechanism involving inhibition of tubulin polymerization.