Author(s): Shirai R, Takayama H, Nishikawa A, Koiso Y, Hashimoto Y
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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.
This article was published in Bioorg Med Chem Lett
and referenced in Journal of Theoretical and Computational Science