Highly potent triazole-based tubulin polymerization inhibitors

Q Zhang, Y Peng, XI Wang, SM Keenan…

文献索引：Zhang, Qiang; Peng, Youyi; Wang, Xin I.; Keenan, Susan M.; Arora, Sonia; Welsh, William J. Journal of Medicinal Chemistry, 2007 , vol. 50, # 4 p. 749 - 754

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被引用次数: 130

摘要

We describe the synthesis and biological evaluation of a series of tubulin polymerization inhibitors that contain the 1, 2, 4-triazole ring to retain the bioactive configuration afforded by the cis double bond in combretastatin A-4 (CA-4). Several of the subject compounds exhibited potent tubulin polymerization inhibitory activity as well as cytotoxicity against a variety of cancer cells including multi-drug-resistant (MDR) cancer cell lines. Attachment of ...