Synthesis, biological evaluations, and tubulin binding poses of C-2alpha sulfur linked taxol analogues

  • Bioorg Med Chem Lett. 2007 Jun 1;17(11):3191-4. doi: 10.1016/j.bmcl.2007.03.026.
Lei Wang  1 ,  Ana A Alcaraz ,  Ruth Matesanz ,  Chun-Gang Yang ,  Isabel Barasoain ,  J Fernando Díaz ,  Ye-Zhi Li ,  James P Snyder ,  Wei-Shuo Fang
Affiliations
  • 1. Institute of Materia Medica, Chinese Academy of Medical Sciences, 1 Xian Nong Tan Street, Beijing 100050, PR China.
PMID: 17395465 DOI: 10.1016/j.bmcl.2007.03.026
Abstract

In combination with chemical modifications, bioassays, and computational simulation techniques, C-2 benzoylthio, and benzylthio taxoids were synthesized, biologically evaluated, and their binding conformations rationalized, in order to probe the interaction of taxane molecule with beta-tubulin.