SYNTHESIS AND EVALUATION OF CYTOTOXICITY OF NOVEL ARYLSULFONYLIMIDAZOLIDINONES CONTAINING SULFONYLUREA PHARMACOPHORE

Design and synthesis of novel 4-phenyl-1-arylsulfonylimidazolones 3 an d 4-phenyl-3-arylsulfonylimidazolones 4 and evaluation of their cytoto xic activity against eleven human cancer cell lines and two murine leu kemia cell lines in vitro were performed. As a result, a series of 4-p henyl-1(N)-arylsulfonylimidazolones (3) has been found to be the poten tial anticancer agent. Compounds 3b, 3c, and 3d exhibit strong activit y as indicated by their IC50 values 0.39, 3.19, 0.31 mu g/mL against A 549 and 0.80, 0.48, 0.0907 mu g/mL against SK-Mel-2, respectively. The se compounds also possess much more potent activity (10-1000 times) th an LY186641 against eleven other cell lines.