Identification of novel, potent and selective inhibitors of Polo-like kinase 1

…, G Naderi-Oboodi, JF Boylan, T Nevins, W Qing…

文献索引：Chen, Shaoqing; Bartkovitz, David; Cai, Jianping; Chen, Yi; Chen, Zhi; Chu, Xin-Jie; Le, Kang; Le, Nam T.; Luk, Kin-Chun; Mischke, Steve; Naderi-Oboodi, Goli; Boylan, John F.; Nevins, Tom; Qing, Weiguo; Chen, Yingsi; Wovkulich, Peter M. Bioorganic and Medicinal Chemistry Letters, 2012 ,  vol. 22,  # 2  p. 1247 - 1250

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被引用次数: 15

摘要

A series of pyrimidodiazepines was identified as potent Polo-like kinase 1 (PLK1) inhibitors. The synthesis and SAR are discussed. The lead compound 7 (RO3280) has potent inhibitory activity against PLK1, good selectivity against other kinases, and excellent in vitro cellular potency. It showed strong antitumor activity in xenograft mouse models.