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Identification of selective inhibitors of cyclin dependent kinase 4 |
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| Authors: | Carini D J Kaltenbach R F Liu J Benfield P A Boylan J Boisclair M Brizuela L Burton C R Cox S Grafstrom R Harrison B A Harrison K Akamike E Markwalder J A Nakano Y Seitz S P Sharp D M Trainor G L Sielecki T M |
| Affiliation: | DuPont Pharmaceuticals Company, Wilmington, DE 19880, USA. thais.m.sielecki@dupontpharma.com |
| Abstract: | A new structural type of kinase inhibitor, containing a benzocarbazole nucleus, has been identified. Members of the series are selective for inhibition of the cyclin dependent kinase family of enzymes. Although the cdks are highly homologous, representatives of the series showed intra-cdk selectivities, especially for cdk4. SAR studies elucidated the important features of the molecules for inhibition. |
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