Synthesis and biological evaluation of novel 1,6-diaryl pyridin-2(1H)-one analogs

Eur J Med Chem. 2013 Jun:64:613-20. doi: 10.1016/j.ejmech.2013.04.008. Epub 2013 Apr 11.

Abstract

A series of 1,6-diaryl pyridin-2(1H)-one analogs were designed and synthesized via consecutive Chan-Lam coupling and Suzuki coupling. These novel compounds were evaluated for their antiproliferative activity against two tumor cell lines (SKOV-3 and HepG2). Compounds 1b, 1c, 1e and 1f displayed comparable in vitro cytotoxicity with taxol, while their in vivo antitumor activity was less effective than taxol. In addition, cell cycle assay indicated that these 1,6-diaryl pyridin-2(1H)-one compounds induced cell cycle arrest in the G1/M phase in the HepG2 cell line.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Cycle / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Hep G2 Cells
  • Humans
  • Mice
  • Molecular Structure
  • Neoplasms, Experimental / drug therapy*
  • Neoplasms, Experimental / pathology
  • Pyridones / chemical synthesis
  • Pyridones / chemistry
  • Pyridones / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Pyridones