Discovery of [4-amino-2-(1-methanesulfonylpiperidin-4-ylamino) pyrimidin-5-yl](2, 3-difluoro-6-methoxyphenyl) methanone (R547), a potent and selective cyclin- …

…, K Packman, C Lukacs, Q Ding, N Jiang…

文献索引：Chu, Xin-Jie; DePinto, Wanda; Bartkovitz, David; So, Sung-Sau; Vu, Binh T.; Packman, Kathryn; Lukacs, Christine; Ding, Qingjie; Jiang, Nan; Wang, Ka; Goelzer, Petra; Yin, Xuefeng; Smith, Melissa A.; Higgins, Brian X.; Chen, Yingsi; Xiang, Qing; Moliterni, John; Kaplan, Gerald; Graves, Bradford; Lovey, Allen; Fotouhi, Nader Journal of Medicinal Chemistry, 2006 , vol. 49, # 22 p. 6549 - 6560

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被引用次数: 97

摘要

The cyclin-dependent kinases (CDKs) and their cyclin partners are key regulators of the cell cycle. Since deregulation of CDKs is found with high frequency in many human cancer cells, pharmacological inhibition of CDKs with small molecules has the potential to provide an effective strategy for the treatment of cancer. The 2, 4-diamino-5-ketopyrimidines 6 reported here represent a novel class of potent and ATP-competitive inhibitors that selectively ...