Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 1, Issue 5, Pages 204-208Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml100051d
Keywords
Cyclin-dependent kinase; oncology therapeutics; SCH 727965
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Inhibition of cyclin-dependent kinases (CDKs) has emerged as an attractive strategy for the development of novel oncology therapeutics. Herein is described the utilization of an in vivo screening approach with integrated efficacy and tolerability parameters to identify candidate CDK inhibitors with a suitable balance of activity and tolerability. This approach has resulted in the identification of SCH 727965, a potent and selective CDK inhibitor that is currently undergoing clinical evaluation.
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