Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors

Bioorg Med Chem Lett. 2004 Aug 2;14(15):3925-8. doi: 10.1016/j.bmcl.2004.05.088.

Abstract

The synthesis of novel aza-1,7-annulated indoles was achieved and these were converted to indolocarbazoles that proved to be potent kinase inhibitors. These compounds were also evaluated in a human colon carcinoma cell line and proved to be good antiproliferative agents.

MeSH terms

  • Aza Compounds / chemical synthesis*
  • Aza Compounds / pharmacology
  • Binding Sites
  • CDC2-CDC28 Kinases / antagonists & inhibitors*
  • CDC2-CDC28 Kinases / chemistry
  • Cell Cycle / drug effects
  • Cyclin-Dependent Kinase 2
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology
  • Indoles / chemical synthesis*
  • Indoles / pharmacology
  • Models, Molecular
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Aza Compounds
  • Enzyme Inhibitors
  • Indoles
  • CDC2-CDC28 Kinases
  • Cyclin-Dependent Kinase 2