Discovery of CYT997: a structurally novel orally active microtubule targeting agent

  • Bioorg Med Chem Lett. 2009 Aug 15;19(16):4639-42. doi: 10.1016/j.bmcl.2009.06.079.
Christopher J Burns  1 ,  Michael F Harte ,  Xianyong Bu ,  Emmanuelle Fantino ,  Max Joffe ,  Harrison Sikanyika ,  Stephen Su ,  C Elisabet Tranberg ,  Neil Wilson ,  Susan A Charman ,  David M Shackleford ,  Andrew F Wilks
Affiliations
  • 1. Cytopia Research Pty Ltd, Richmond, VIC 3121, Australia.
PMID: 19616947 DOI: 10.1016/j.bmcl.2009.06.079
Abstract

CYT997 was discovered as a potent tubulin polymerization inhibitor possessing potent cytotoxic activity against a range of Cancer cells. Details of SAR studies, pharmacokinetic investigations and synthesis of compounds leading to the discovery of CYT997 are reported.