Design, synthesis and aromatase inhibitory activities of novel indole-imidazole derivatives

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1760-2. doi: 10.1016/j.bmcl.2013.01.045. Epub 2013 Jan 26.

Abstract

A series of novel indole-imidazole derivatives have been prepared and evaluated in vitro on the aromatase inhibitory activities. The results suggested that proton or a small electron-withdrawing group at para-position of the phenyl ring would enhance the inhibitory activities and any bulky group should be avoided in order to keep a relative small volume for this kind of molecules.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aromatase / chemistry*
  • Aromatase / metabolism
  • Aromatase Inhibitors / chemical synthesis*
  • Aromatase Inhibitors / chemistry
  • Aromatase Inhibitors / metabolism
  • Crystallography, X-Ray
  • Drug Design*
  • Imidazoles / chemical synthesis
  • Imidazoles / chemistry*
  • Imidazoles / metabolism
  • Indoles / chemistry*
  • Molecular Conformation
  • Protein Binding
  • Structure-Activity Relationship

Substances

  • Aromatase Inhibitors
  • Imidazoles
  • Indoles
  • imidazole
  • indole
  • Aromatase