Regioselective one pot synthesis of 3,3'-diindolylethylene derivatives and study of their cytotoxic activity

Bioorg Med Chem Lett. 2011 May 15;21(10):3084-7. doi: 10.1016/j.bmcl.2011.03.028. Epub 2011 Mar 16.

Abstract

2,2'-Diphenyl-3,3'-diindolylethylene (DPDIE) derivatives 3a-g were regioselectively prepared in one pot from indoles 1a-g in the presence of Lewis acids and were subsequently evaluated for cytotoxic activity against human leukemic cell lines, U937 and K562. The most potent compound 3g exhibited IC(50) of 13.0-17.0 μM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / toxicity*
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Crystallography, X-Ray
  • Ethylenes / chemical synthesis*
  • Ethylenes / chemistry
  • Ethylenes / pharmacology*
  • Flow Cytometry
  • Humans
  • Indoles / chemistry*
  • Inhibitory Concentration 50
  • Molecular Structure

Substances

  • Antineoplastic Agents
  • Ethylenes
  • Indoles
  • ethylene