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.

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