2. Academic Validation
  3. Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles

Novel, potent and selective cyclin D1/CDK4 inhibitors: indolo[6,7-a]pyrrolo[3,4-c]carbazoles

  • Bioorg Med Chem Lett. 2003 Jul 21;13(14):2261-7. doi: 10.1016/s0960-894x(03)00461-x.
Thomas A Engler 1,  Kelly Furness,  Sushant Malhotra,  Concha Sanchez-Martinez,  Chuan Shih,  Walter Xie,  Guoxin Zhu,  Xun Zhou,  Scott Conner,  Margaret M Faul,  Kevin A Sullivan,  Stanley P Kolis,  Harold B Brooks,  Bharvin Patel,  Richard M Schultz,  Tammy B DeHahn,  Kashif Kirmani,  Charles D Spencer,  Scott A Watkins,  Eileen L Considine,  Jack A Dempsey,  Catherine A Ogg,  Nancy B Stamm,  Bryan D Anderson,  Robert M Campbell,  Vasu Vasudevan,  Michelle L Lytle
Affiliations

Affiliation

  • 1 Lilly Research Laboratories, Eli Lilly and Company, 46285, Indianapolis, IN, USA. [email protected]
PMID: 12824014 DOI: 10.1016/s0960-894x(03)00461-x
Abstract

The synthesis and CDK inhibitory properties of a series of indolo[6,7-a]pyrrolo[3,4-c]carbazoles is reported. In addition to their potent CDK activity, the compounds display antiproliferative activity against two human Cancer cell lines. These inhibitors also effect strong G1 arrest in these cell lines and inhibit Rb phosphorylation at Ser780 consistent with inhibition of cyclin D1/CDK4.

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