- Identification of novel, potent and selective inhibitors of Polo-like kinase 1.
Identification of novel, potent and selective inhibitors of Polo-like kinase 1.
Bioorganic & medicinal chemistry letters (2011-12-17)
Shaoqing Chen, David Bartkovitz, Jianping Cai, Yi Chen, Zhi Chen, Xin-Jie Chu, Kang Le, Nam T Le, Kin-Chun Luk, Steve Mischke, Goli Naderi-Oboodi, John F Boylan, Tom Nevins, Weiguo Qing, Yingsi Chen, Peter M Wovkulich
PMID22172702
RÉSUMÉ
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.
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