1,7-annulated indolocarbazoles as cyclin-dependent kinase inhibitors

Rima S Al-awar; James E Ray; Kyle A Hecker; Jianping Huang; Philip P Waid; Chuan Shih; Harold B Brooks; Charles D Spencer; Scott A Watkins; Bharvin R Patel; Nancy B Stamm; Catherine A Ogg; Richard M Schultz; Eileen L Considine; Margaret M Faul; Kevin A Sullivan; Stanley P Kolis; John L Grutsch; Sajan Joseph

doi:10.1016/j.bmcl.2004.03.105

1,7-annulated indolocarbazoles as cyclin-dependent kinase inhibitors

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3217-20. doi: 10.1016/j.bmcl.2004.03.105.

Affiliation

¹ Discovery Chemistry Research, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA. rima@lilly.com

PMID: 15149678
DOI: 10.1016/j.bmcl.2004.03.105

Abstract

The synthesis and kinase inhibitory activity of a series of novel 1,7-annulated indolocarbazoles 6 and 16 is described. These compounds exhibited potent inhibitory activity against cyclin-dependent kinase 4 and good antiproliferative activity in a human colon carcinoma cell line.

MeSH terms

Carbazoles / chemistry*
Carbazoles / pharmacology
Cyclin D1 / antagonists & inhibitors
Cyclin D1 / metabolism
Cyclin-Dependent Kinase 4
Cyclin-Dependent Kinases / antagonists & inhibitors*
Cyclin-Dependent Kinases / metabolism
Indoles / chemistry*
Indoles / pharmacology
Protein Kinase Inhibitors / chemistry*
Protein Kinase Inhibitors / pharmacology
Proto-Oncogene Proteins / antagonists & inhibitors
Proto-Oncogene Proteins / metabolism

Substances

Carbazoles
Indoles
Protein Kinase Inhibitors
Proto-Oncogene Proteins
Cyclin D1
Cyclin-Dependent Kinase 4
Cyclin-Dependent Kinases