2. Academic Validation
  3. Asymmetric synthesis of antimitotic combretadioxolane with potent antitumor activity against multi-drug resistant cells

Asymmetric synthesis of antimitotic combretadioxolane with potent antitumor activity against multi-drug resistant cells

  • Bioorg Med Chem Lett. 1998 Aug 4;8(15):1997-2000. doi: 10.1016/s0960-894x(98)00344-8.
R Shirai 1,  H Takayama,  A Nishikawa,  Y Koiso,  Y Hashimoto
Affiliations

Affiliation

  • 1 Institute of Molecular and Cellular Biosciences (IMCB), University of Tokyo, Japan.
PMID: 9873473 DOI: 10.1016/s0960-894x(98)00344-8
Abstract

The (S,S)-enantiomer of combretadioxolane (3), designed as a chirally preorganized derivative of combretastatin A-4, exhibited quite strong tubulin polymerization-inhibitory activity (IC50: 4-6 microM). (S,S)-3 is 20 times more potent than vincristine as an in vitro growth inhibitor (in terms of GI50) of the multi-drug-resistant (MDR) cell line PC-12, which produces P-glycoprotein.

Figures