| Literature DB >> 12747775 |
Guoxin Zhu1, Scott E Conner, Xun Zhou, Chuan Shih, Tiechao Li, Bryan D Anderson, Harold B Brooks, Robert Morris Campbell, Eileen Considine, Jack A Dempsey, Margaret M Faul, Cathy Ogg, Bharvin Patel, Richard M Schultz, Charles D Spencer, Beverly Teicher, Scott A Watkins.
Abstract
Novel substituted indolocarbazoles were synthesized, and their kinase inhibitory capability was evaluated in vitro. 6-Substituted indolocarbazoles 4 were found to be potent and selective D1/CDK4 inhibitors. 4d and 4h exhibited potent and ATP-competitive D1/CDK4 activities with IC50 values of 76 and 42 nM, respectively. Both compounds had high selectivity against the other kinases. These D1/CDK4 inhibitors inhibited tumor cell growth, arrested tumor cells at the G1 phase, and inhibited pRb phosphorylation.Entities:
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Year: 2003 PMID： 12747775 DOI： 10.1021/jm0256169
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446