PLANAR STRUCTURAL REQUIREMENT AT 4-POSITION OF 1-ARYLSULFONYL-4-PHENYL-4,5-DIHYDRO-2-IMIDAZOLONES FOR THEIR CYTOTOXICITY

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