Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 24, Pages 6486-6489Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.10.075
Keywords
Kinase; Cyclin-dependent kinase; Kinase inhibitor; Imidazole amide; CDK; Cell cycle; Cancer
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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 hERG potassium ion channel. A compound with an attractive overall balance of properties was pro. led in vivo and possessed suitable physiochemical and pharmacokinetic profiles for oral dosing. (C) 2008 Elsevier Ltd. All rights reserved.
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