Asymmetric synthesis of antimitotic combretadioxolane with potent antitumor activity against multi-drug resistant cells.
作者信息
Shirai R, Takayama H, Nishikawa A, Koiso Y, Hashimoto Y
机构信息
Institute of Molecular and Cellular Biosciences (IMCB), University of Tokyo, Japan.
出版信息
Bioorg Med Chem Lett. 1998 Aug 4;8(15):1997-2000. doi: 10.1016/s0960-894x(98)00344-8.
PMID:9873473
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.
摘要
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