Synthesis of 1,7-annulated indoles and their applications in the studies of cyclin dependent kinase inhibitors

Guoxin Zhu; Scott E Conner; Xun Zhou; Ho-Kit Chan; Chuan Shih; Thomas A Engler; Rima S Al-Awar; Harold B Brooks; Scott A Watkins; Charles D Spencer; Richard M Schultz; Jack A Dempsey; Eileen L Considine; Bharvin R Patel; Catherine A Ogg; Vasu Vasudevan; Michelle L Lytle

doi:10.1016/j.bmcl.2004.04.033

Synthesis of 1,7-annulated indoles and their applications in the studies of cyclin dependent kinase inhibitors

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3057-61. doi: 10.1016/j.bmcl.2004.04.033.

Authors

Guoxin Zhu¹, Scott E Conner, Xun Zhou, Ho-Kit Chan, Chuan Shih, Thomas A Engler, Rima S Al-Awar, Harold B Brooks, Scott A Watkins, Charles D Spencer, Richard M Schultz, Jack A Dempsey, Eileen L Considine, Bharvin R Patel, Catherine A Ogg, Vasu Vasudevan, Michelle L Lytle

Affiliation

¹ Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA. [email protected]

PMID: 15149644
DOI: 10.1016/j.bmcl.2004.04.033

Abstract

The synthesis of a novel series of 1,7-annulated indolocarbazoles 2 and 16 is described. These compounds were found to be potent cyclin dependent kinase inhibitors with good antiproliferative activity against two human carcinoma cell lines. These inhibitors also arrested tumor cells at the G1 phase and inhibited pRb phosphorylation.

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / pharmacology
Cell Line, Tumor
Cyclin-Dependent Kinases / antagonists & inhibitors*
Cyclin-Dependent Kinases / metabolism
Growth Inhibitors / chemical synthesis
Growth Inhibitors / pharmacology
Humans
Indoles / chemical synthesis*
Indoles / pharmacology
Protein Kinase Inhibitors / chemical synthesis*
Protein Kinase Inhibitors / pharmacology

Substances

Antineoplastic Agents
Growth Inhibitors
Indoles
Protein Kinase Inhibitors
Cyclin-Dependent Kinases