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KMID : 0043319970200030283
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Archives of Pharmacal Research
1997 Volume.20 No. 3 p.283 ~ p.287
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Planar Structural Requirement at 4-position of 1-Arylsulfonyl-4-phenyl-4,5-dihydro-2-imidazolones for their Cytotoxicity
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Jung Sang-Hun
Kwak Suhk-Jun
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Abstract
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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.
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KEYWORD
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Cytotoxic activicity, 4-phenyl-1-arylsulfonylimidazolone, Phenyl pharmacophore
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