A novel pyrazolo [1, 5-a] pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor …

…, M Periyasamy, M Alikian, SK Kanneganti…

文献索引：Heathcote, Dean A.; Patel, Hetal; Kroll, Sebastian H. B.; Hazel, Pascale; Periyasamy, Manikandan; Alikian, Mary; Kanneganti, Seshu K.; Jogalekar, Ashutosh S.; Scheiper, Bodo; Barbazanges, Marion; Blum, Andreas; Brackow, Jan; Siwicka, Alekasandra; Pace, Robert D. M.; Fuchter, Matthew J.; Snyder, James P.; Liotta, Dennis C.; Freemont, Paul. S.; Aboagye, Eric O.; Coombes, R. Charles; Barrett, Anthony G. M.; Ali, Simak Journal of Medicinal Chemistry, 2010 , vol. 53, # 24 p. 8508 - 8522

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被引用次数: 30

摘要

Cyclin-dependent protein kinases (CDKs) are central to the appropriate regulation of cell proliferation, apoptosis, and gene expression. Abnormalities in CDK activity and regulation are common features of cancer, making CDK family members attractive targets for the development of anticancer drugs. Here, we report the identification of a pyrazolo [1, 5-a] pyrimidine derived compound, 4k (BS-194), as a selective and potent CDK inhibitor, which ...