Discovery of highly potent and selective pan-Aurora kinase inhibitors with enhanced in vivo antitumor therapeutic index

…, TD Vickers, S Xu, MJ Hadd, S Quiambao…

文献索引：Liu, Gang; Abraham, Sunny; Tran, Lan; Vickers, Troy D.; Xu, Shimin; Hadd, Michael J.; Quiambao, Sheena; Holladay, Mark W.; Hua, Helen; Ford Pulido, Julia M.; Gunawardane, Ruwanthi N.; Davis, Mindy I.; Eichelberger, Shawn R.; Apuy, Julius L.; Gitnick, Dana; Gardner, Michael F.; James, Joyce; Breider, Mike A.; Belli, Barbara; Armstrong, Robert C.; Treiber, Daniel K. Journal of Medicinal Chemistry, 2012 , vol. 55, # 7 p. 3250 - 3260

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被引用次数: 6

摘要

Serine/threonine protein kinases Aurora A, B, and C play essential roles in cell mitosis and cytokinesis. Currently a number of Aurora kinase inhibitors with different isoform selectivities are being evaluated in the clinic. Herein we report the discovery and characterization of 21c (AC014) and 21i (AC081), two structurally novel, potent, kinome-selective pan-Aurora inhibitors. In the human colon cancer cell line HCT-116, both compounds potently inhibit ...