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Identification of Novel, Potent and Selective Inhibitors of Polo-like Kinase 1

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

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1247-50.

PMID: 22172702

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP1062243519 RO3280 RO3280 1062243-51-9 Price
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