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 1-arylsulfonyl-4-phenyl-4,5-dihydro-2-limidazolones3 for their cytotoxicity, the corresponding 1-arylsulfonyl-4-cyclohexyl-4,5-dihydro-2-imidazolones4 were synthesized and theirin vitro cytotoxicity against human solid tumor cell lines were measured. Unlike compounds3a-c, cyclohexyl analogues4a-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-phenyl-4,5-dihydro-2-limidazolones3 is required for their activity as an important pharmacophoric moiety.
Jung
S H
SH
College of Pharmacy, Chung-Nam National University, 305-764, Taejon, Korea.
Kwak
S J
SJ