Syntheses and antiproliferative evaluation of oxyphenisatin derivatives

  • Bioorg Med Chem Lett. 2007 May 15;17(10):2854-7. doi: 10.1016/j.bmcl.2007.02.060.
Muhammed K Uddin  1 ,  Serge G Reignier ,  Tom Coulter ,  Christian Montalbetti ,  Charlotta Grånäs ,  Steven Butcher ,  Christian Krog-Jensen ,  Jakob Felding
Affiliations
  • 1. Evotec(UK) Ltd, 111 Milton Park, Abingdon, Oxon OX14 4RX, UK.
PMID: 17368900 DOI: 10.1016/j.bmcl.2007.02.060
Abstract

Syntheses and structure-antiproliferative relationship for oxyphenisatin analogues are described. The cell proliferation data showed that the presence of substituents (especially F, Cl, Me, CF(3), and OMe) in the 6- and 7-position of oxyphenisatin markedly enhanced the potency in the MDA-468 cell line without affecting the MDA-231 cell line. The best compounds from this series showed low nanomolar antiproliferative activity towards the MDA-468 cell line and a 1000-fold selectivity over the MDA-231 cell line.