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Asymmetric synthesis of antimitotic combretadioxolane with potent antitumor activity against multi-drug resistant
R Shirai1, H Takayama, A Nishikawa
1Institute of Molecular and Cellular Biosciences (IMCB), University of Tokyo, Japan.
Bioorganic & Medicinal Chemistry Letters
|January 5, 1999
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.