A novel, broad-spectrum anticancer compound containing the imidazo[4,5-e][1,3]diazepine ring system

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4386-9. doi: 10.1016/j.bmcl.2010.06.061. Epub 2010 Jun 15.

Abstract

Synthesis and broad-spectrum anticancer activity of a novel heterocyclic compound 1 containing the title imidazo[4,5-e][1,3]diazepine ring system have been reported. The compound shows potent in vitro antitumor activity with low micromolar IC(50)'s against prostate, lung, breast, and ovarian cancer cell lines tested. The long alkyl chain attached to the six-position of the heterocyclic ring of 1 appears to be necessary for the observed biological activity.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / therapeutic use
  • Azepines / chemistry*
  • Breast Neoplasms / drug therapy
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Female
  • Heterocyclic Compounds / chemical synthesis
  • Heterocyclic Compounds / chemistry*
  • Heterocyclic Compounds / therapeutic use
  • Humans
  • Lung Neoplasms / drug therapy
  • Male
  • Neoplasms / drug therapy*
  • Ovarian Neoplasms / drug therapy
  • Prostatic Neoplasms / drug therapy
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Azepines
  • Heterocyclic Compounds