Eco-friendly synthesis and antiproliferative evaluation of some oxygen substituted diaryl ketones

Molecules. 2013 Aug 16;18(8):9818-32. doi: 10.3390/molecules18089818.

Abstract

A broad variety of oxygen-substituted diaryl ketones has been synthesized by solar energy-induced Friedel Crafts acylations of 1,4-benzo- and 1,4-naphthoquinones with benzaldehydes. The in vitro antiproliferative properties of the photoproducts were assessed on prostate (DU-145), bladder (T24) and breast (MCF7) human-derived tumor cell lines and compared to non-tumor mouse fibroblasts (Balb/3T3). Among the tested compounds, it was found that those containing a 3,4,5-trimethoxyphenyl A-ring, such as 12 and 22 are more active on DU-145, with EC50 values of 1.2 and 5.9 μM, respectively. By comparing their effects on the three cancer cell lines, the analogue 22 has the best mean selective index (2.4).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Drug Screening Assays, Antitumor
  • Humans
  • Ketones / chemistry*
  • Ketones / pharmacology*
  • Mice
  • Molecular Structure
  • Oxygen / chemistry*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Ketones
  • Oxygen