Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors

…, C Geh, CP Green, M Johannsen, M Walker…

Index: Jones, Clifford D.; Andrews, David M.; Barker, Andrew J.; Blades, Kevin; Byth, Kate F.; Finlay, M. Raymond V.; Geh, Catherine; Green, Clive P.; Johannsen, Marie; Walker, Mike; Weir, Hazel M. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 24 p. 6486 - 6489

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Citation Number: 21

Abstract

The development of a novel series of imidazole pyrimidine amides as cyclin-dependent kinase (CDK) inhibitors is described. The series was found to have much improved CDK2 inhibition and potent in vitro anti-proliferative effects against cancer cell lines. Control of overall lipophilicity was important to achieve good in vitro potency along with acceptable physiochemical properties and margins against inhibition of both CYP isoforms and the ...