Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors

…, CA Brassington, J Breed, KF Byth, JD Culshaw…

Index: Anderson, Malcolm; Andrews, David M.; Barker, Andy J.; Brassington, Claire A.; Breed, Jason; Byth, Kate F.; Culshaw, Janet D.; Finlay, M. Raymond V.; Fisher, Eric; McMiken, Helen H.J.; Green, Clive P.; Heaton, Dave W.; Nash, Ian A.; Newcombe, Nicholas J.; Oakes, Sandra E.; Pauptit, Richard A.; Roberts, Andrew; Stanway, Judith J.; Thomas, Andrew P.; Tucker, Julie A.; Walker, Mike; Weir, Hazel M. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 20 p. 5487 - 5492

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Citation Number: 27

Abstract

An imidazole series of cyclin-dependent kinase (CDK) inhibitors has been developed. Protein inhibitor structure determination has provided an understanding of the emerging structure activity trends for the imidazole series. The introduction of a methyl sulfone at the aniline terminus led to a more orally bioavailable CDK inhibitor that was progressed into clinical development.