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

DOI: 10.1016/S0960-894X(98)00344-8

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 1997 - 2000 (1998)

Update date:2022-08-04

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Authors:

Shirai, Ryuichi

Takayama, Hisae

Nishikawa, Asuka

Koiso, Yukiko

Hashimoto, Yuichi

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Article abstract of DOI:10.1016/S0960-894X(98)00344-8

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.

Full text of DOI:10.1016/S0960-894X(98)00344-8

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