Multisubstituted indole-acrylonitrile hybrids as potential cytotoxic agents

Bioorg Med Chem Lett. 2014 Apr 15;24(8):1907-11. doi: 10.1016/j.bmcl.2014.03.011. Epub 2014 Mar 17.

Abstract

A series of multisubstituted indole-acrylonitrile hybrids were designed, synthesized and evaluated for their potential cytotoxic activities. The bio-evaluation results indicated that some of the target compounds (such as 3a, 3f, 3k, 3n) exhibited good to moderate cytotoxic effect on HepG2, BCG-823, BEL-7402, and HL-7702 cell lines. Especially, the compounds 3a and 3k also exhibited high cytotoxic activities (3a, 19.38±3.38 μM; 3k, 15.43±3.54 μM) against the BEL-7402 cell line resistant to Taxol (>25μM) and 5-FU (>500 μM), which might be developed as novel lead scaffold for potential anticancer agents.

Keywords: Cytotoxic activity; Hybrids; Multisubstituted indole–acrylonitrile; Synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylonitrile* / chemistry
  • Acrylonitrile* / toxicity
  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / toxicity
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Cytotoxins* / chemistry
  • Cytotoxins* / toxicity
  • Drug Resistance, Neoplasm / drug effects
  • Drug Screening Assays, Antitumor
  • Hep G2 Cells
  • Humans
  • Indoles* / chemistry
  • Indoles* / toxicity
  • Inhibitory Concentration 50
  • Molecular Structure

Substances

  • Antineoplastic Agents
  • Cytotoxins
  • Indoles
  • indole
  • Acrylonitrile