Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues

Bioorg Med Chem Lett. 2008 Feb 1;18(3):989-93. doi: 10.1016/j.bmcl.2007.12.023. Epub 2007 Dec 15.

Abstract

A series of new 1,4-diarylimidazol-2(3H)-one derivatives and their 2-thione analogues has been prepared and evaluated in vitro for antitumor activity against the NCI human cancer cell panel. Compounds bearing a 3,4,5-trimethoxyphenyl ring linked to either N-1 or C-4 position of the imidazole core demonstrated an interesting profile of cytotoxicity with preferential activity against leukemic cell lines. Compound 13 exhibited a potent antitumor activity against MOLT-4 (GI(50)=20 nM) and SR (GI(50)=32 nM) cell lines.

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Drug Design*
  • Drug Screening Assays, Antitumor
  • Humans
  • Imidazoles / chemical synthesis*
  • Imidazoles / chemistry
  • Imidazoles / pharmacology*
  • Molecular Structure
  • Structure-Activity Relationship
  • Thiones / chemical synthesis*
  • Thiones / chemistry
  • Thiones / pharmacology*
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Imidazoles
  • Thiones