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  • Title: Potent Antitumor Activities and Structure Basis of the Chiral β-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin.
    Author: Zhou P, Liu Y, Zhou L, Zhu K, Feng K, Zhang H, Liang Y, Jiang H, Luo C, Liu M, Wang Y.
    Journal: J Med Chem; 2016 Nov 23; 59(22):10329-10334. PubMed ID: 27805821.
    Abstract:
    A series of chiral β-lactam bridged analogues (3-substituted 1,4-diaryl-2-azetidinones) of combretastatin A-4 (CA-4) were synthesized asymmetrically, and their antitumor activities were evaluated in vitro and in vivo. The cocrystal structure of tubulin in complex with compound 9 was determined by X-ray crystallography, which showed that 9 binds to the same site as colchicine with similar binding mode, and the absolute configuration of its C-4 was first identified and demonstrated to be critically important for their antiproliferative activities.
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