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

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 (GI50 = 20 nM) and SR (GI50 = 32 nM) cell lines.

Graphical abstractThe synthesis and in vitro antitumor activity against the NCI 60 cell line panel of new 1,4-diarylimidazol-2(3H)-one derivatives and their 2-thione analogues is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide