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Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6

…, T Zhu, J Brodfuehrer, C Choi, MR Barvian…

文献索引:Toogood, Peter L.; Harvey, Patricia J.; Repine, Joseph T.; Sheehan, Derek J.; VanderWel, Scott N.; Zhou, Hairong; Keller, Paul R.; McNamara, Dennis J.; Sherry, Debra; Zhu, Tong; Brodfuehrer, Joanne; Choi, Chung; Barvian, Mark R.; Fry, David W. Journal of Medicinal Chemistry, 2005 , vol. 48, # 7 p. 2388 - 2406

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被引用次数: 231

摘要

A pharmacological approach to inhibition of cyclin-dependent kinases 4 and 6 (Cdk4/6) using highly selective small molecule inhibitors has the potential to provide novel cancer therapies for clinical use. Achieving high levels of selectivity for Cdk4/6, versus other ATP- dependent kinases, presents a significant challenge. The pyrido [2, 3-d] pyrimidin-7-one template provides an effective platform for the inhibition of a broad cross-section of ...