Bio-inspired synthesis and biological evaluation of a colchicine-related compound library

  • Bioorg Med Chem Lett. 2012 Jun 1;22(11):3776-80. doi: 10.1016/j.bmcl.2012.04.007.
K C Nicolaou  1 ,  Roman A Valiulin ,  Jonathan K Pokorski ,  Vicki Chang ,  Jason S Chen
Affiliations
  • 1. Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA. [email protected]
PMID: 22542017 DOI: 10.1016/j.bmcl.2012.04.007
Abstract

A bio-inspired investigation of the reactions of substrates of type 1 with VOF(3) and PIFA [phenyliodine(III) bis(trifluoroacetate)] led to a collection of colchicine-like compounds 2-5 and related systems. Biological evaluation revealed that some of the synthesized products had significant cytotoxic properties against the colon Cancer cell line HT-29.