Synthesis and biological evaluation of chalcones and their derived pyrazoles as potential cytotoxic agents

Bioorg Med Chem Lett. 2005 Jun 15;15(12):3177-80. doi: 10.1016/j.bmcl.2005.03.121.

Abstract

A series of substituted chalcones and their corresponding pyrazoles were synthesized and evaluated for in vitro cytotoxic activity against a panel of human cancer cell lines. Out of 93 compounds screened, 8 compounds, 1s, 3i,j,n, 4i,j,n and 4s, showed marked activity. Compounds 4j,n and 4s were found to be the most promising in this study. SAR is also discussed.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Chalcone / chemical synthesis
  • Chalcone / chemistry*
  • Chalcone / pharmacology*
  • Drug Screening Assays, Antitumor
  • Humans
  • Inhibitory Concentration 50
  • Neoplasms / drug therapy
  • Pyrazoles / chemical synthesis
  • Pyrazoles / chemistry*
  • Pyrazoles / pharmacology*
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Pyrazoles
  • Chalcone