• Archives of Pharmacal Research
• /
• v.20 no.3
• /
• pp.283-287
• /
• 1997

In order to identify the structural requirement at 4-position of 1-arylsulfonyl-4-phenyl-4,5-dihydro-2-limidazolones 3 for their cytotoxicity, the corresponding 1-arylsulfonyl-4-cyclohexyl-4,5-dihydro-2-imidazolones 4 were synthesized and their in vitro cytotoxicity against human solid tumor cell lines were measured. Unlike compounds 3a-c, cyclohexyl analogues 4a-c do not show the cytotoxicity. This dramatic loss of activity of these analogues on the volume change with the bulkier cyclohexyl group indicates that the planar structure at 4-position of 1-arylsulfonyl-4-pheny-4,5-dihydro-2-limidazolones 3 is required for their activity as an important pharmacophoric moiety.

• Archives of Pharmacal Research
• /
• v.19 no.6
• /
• pp.570-580
• /
• 1996

Design and synthesis of novel 4-phenyl-1-arylsulfonylimidazolones 3 and 4-phenyl-3-arylsulfonylimidazolones 4 and evaluation of their cytotoxic activity against eleven human cancer cell lines and two murine leukemia cell lines in vitro were performed. As a result, a series of 4-phenyl-1(N)-arylsulfonylimidazolones (3) has been found to be the potential anticancer agent. Compounds 3b, 3c, and 3d exhibit strong activity as indicated by their $IC_{50}$ values 0.39, 3.19, $0.31{\mu}g/mL$ against A549 and 0.80, 0.48, $0.0007{\mu}g/mL$against SK-Mel-2, respectively. These compounds also possess much more potent activity (10-1000 times) than LY186641 against eleven other cell lines.