Bioorganic and Medicinal Chemistry Letters p. 1997 - 2000 (1998)
Update date:2022-08-04
Topics:
Shirai, Ryuichi
Takayama, Hisae
Nishikawa, Asuka
Koiso, Yukiko
Hashimoto, Yuichi
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 μM). (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.
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(2010)
