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…

Index: 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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Citation Number: 30

Abstract

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 ...