Investigation of N-Arylsulfonylimidazole as Novel Scaffold for Anticancer Agents

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dc.contributor.authorS Subramanian-
dc.contributor.authorH S Yang-
dc.contributor.authorM Manickam-
dc.contributor.authorJieun Yun-
dc.contributor.authorS H Jung-
dc.date.accessioned2017-04-19T10:30:53Z-
dc.date.available2017-04-19T10:30:53Z-
dc.date.issued2016-
dc.identifier.issn02532964-
dc.identifier.uri10.1002/bkcs.10734ko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/13587-
dc.description.abstractTo explore the possibility of isosteric replacement of imidazolidinone moiety of (S)-1-(1-(4-aminobenzoyl) indolin-5-ylsulfonyl)-4-phenylimidazolidin-2-one (1) for the anticancer activity, novel 1-(1-acyl substituted indolin-5-sulfonyl)-4-phenyl-1H-imidazoles 2 were prepared with varying the N-acyl group on the indoline ring and evaluated for their in vitro anticancer activity against six human cancer cell lines (renal ACHN, colon HCT-15, breast MDA-MB-231, lung NCI-H23, stomach NUGC-3, and prostrate PC-3). Among the analogs prepared, imidazoles with hydrophobic acyl substituents on indoline like cyclohexanecarbonyl (2e, mean 50% growth inhibition [GI50] = 2.29 μM) or benzoyl with electrondonating groups like 4-methoxybenzoyl (2g, mean GI50 = 4.11 μM) and 4-aminobenzoyl (2a, mean GI50 = 4.45 μM) exhibited relatively good cytotoxicity. Although imidazole moiety of arylsulfonylphenylimidazole 2 contains only hydrogen bonding acceptor property without a stereogenic center unlike imidazolidinone analogs, the high level of the activity of 2 proved that the imidazole motif is obviously good isostere of imidazolidinone moiety of arylsulfonylphenylimidazolidinone 1 for the anticancer activity.-
dc.publisherWiley-
dc.titleInvestigation of N-Arylsulfonylimidazole as Novel Scaffold for Anticancer Agents-
dc.title.alternativeInvestigation of N-Arylsulfonylimidazole as Novel Scaffold for Anticancer Agents-
dc.typeArticle-
dc.citation.titleBulletin of Korean Chemical Society-
dc.citation.number5-
dc.citation.endPage637-
dc.citation.startPage632-
dc.citation.volume37-
dc.contributor.alternativeNameSubramanian-
dc.contributor.alternativeName양현순-
dc.contributor.alternativeNameManickam-
dc.contributor.alternativeName윤지은-
dc.contributor.alternativeName정상헌-
dc.identifier.bibliographicCitationBulletin of Korean Chemical Society, vol. 37, no. 5, pp. 632-637-
dc.identifier.doi10.1002/bkcs.10734-
dc.subject.keywordAnticancer activity-
dc.subject.keywordAntimitotic-
dc.subject.keywordN-arylsulfonylimidazole-
dc.subject.keywordN-arylsulfonylimidazolidinone-
dc.subject.localAnticancer activity-
dc.subject.localAntimitotic-
dc.subject.localN-arylsulfonylimidazole-
dc.subject.localN-arylsulfonylimidazolidinone-
dc.description.journalClassY-
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