Structure–activity relationship study of arylsulfonylimidazolidinones as anticancer agents

In an effort to find novel N-arylsulfonylimidazolidinones as highly potent anticancer agent, the structure–activity relationship of ethyl 2-methyl-4-(2-oxo-4-phenylimidazolidin-1-ylsulfonyl)phenylcarbamate was explored through synthesis and evaluation of in vitro cytotoxicity of its analogs against HCT116, A549 and NCL-H460 cancer cell lines. Among the synthesized derivatives, the carbamate analogs (4a–f and 4k–p) exhibited superior cytotoxicity to doxorubicin for all cancer cell lines. The SAR studies of these derivatives confirm that the intact 4-phenyl-l-benzenesulfonylimidazolidinone has a pivotal role as a basic pharmacophore and hydrophobic substitutions only at 2-position of 1-aminobenzenesulfonyl moiety are beneficial for the enhancement of the activity.

In order to study the SAR of N-arylsulfonylimidazolidinones, a series of its derivatives were designed, synthesized and tested for their cytotoxicity.Figure optionsDownload as PowerPoint slide