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Synthesis and structure–activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors

2005; Elsevier BV; Volume: 15; Issue: 23 Linguagem: Inglês

10.1016/j.bmcl.2005.08.056

1464-3405

Xiaohu Ouyang, Xiaoling Chen, Evgueni L. Piatnitski, Alexander S. Kiselyov, Haiying He, Yunyu Mao, Vatee Pattaropong, Yang Yu, Ki H. Kim, John Kincaid, Leon M. Smith, Wai C. Wong, Sui Ping Lee, Daniel L. Milligan, Asra Malikzay, James Fleming, Jason Gerlak, Dhanvanthri S. Deevi, Jacqueline Doody, Hui-Hsien Chiang, Sheetal Patel, Ying Wang, Robin L. Rolser, Paul Kussie, Marc Labelle, M. Carolina Tuma,

Synthesis and Biological Evaluation

A novel triazole-containing chemical series was shown to inhibit tubulin polymerization and cause cell cycle arrest in A431 cancer cells with EC(50) values in the single digit nanomolar range. Binding experiments demonstrated that representative active compounds of this class compete with colchicine for its binding site on tubulin. The syntheses and structure-activity relationship studies for the triazole derivatives are described herein.