Synthesis of a novel series of 2-alkylthio substituted naphthoquinones as potent acyl-CoA: Cholesterol acyltransferase (ACAT) inhibitors

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dc.contributor.authorK Lee-
dc.contributor.authorS H Cho-
dc.contributor.authorJ H Lee-
dc.contributor.authorJ Goo-
dc.contributor.authorS Y Lee-
dc.contributor.authorS K Boovanahalli-
dc.contributor.authorS K Yeo-
dc.contributor.authorS J Lee-
dc.contributor.authorYoung Kook Kim-
dc.contributor.authorD H Kim-
dc.contributor.authorY Choi-
dc.contributor.authorG Y Song-
dc.date.accessioned2017-04-19T09:36:51Z-
dc.date.available2017-04-19T09:36:51Z-
dc.date.issued2013-
dc.identifier.issn0223-5234-
dc.identifier.uri10.1016/j.ejmech.2013.01.020ko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/11192-
dc.description.abstractWe report a new series of naphthoquinone derivatives as potent ACAT inhibitors, which were obtained through structural variations of previously disclosed lead 1. Several analogs represented by 3i-l, 4k-m, 6a-n, 7a, and 7i demonstrated potent human macrophage ACAT inhibitory activity by a cell-based reporter assay with human HepG2 cell lines. In particular, compounds 4l and 6j emerged as highly potent inhibitors, exhibiting significantly high inhibitory potencies with IC50 values of 0.44 μM and 0.6 μM, respectively. Moreover, compound 4l significantly reduced the accumulation of cellular cholesterol in HepG2 cell lines.-
dc.publisherElsevier-
dc.titleSynthesis of a novel series of 2-alkylthio substituted naphthoquinones as potent acyl-CoA: Cholesterol acyltransferase (ACAT) inhibitors-
dc.title.alternativeSynthesis of a novel series of 2-alkylthio substituted naphthoquinones as potent acyl-CoA: Cholesterol acyltransferase (ACAT) inhibitors-
dc.typeArticle-
dc.citation.titleEuropean Journal of Medicinal Chemistry-
dc.citation.number0-
dc.citation.endPage525-
dc.citation.startPage515-
dc.citation.volume62-
dc.contributor.affiliatedAuthorYoung Kook Kim-
dc.contributor.alternativeName이경-
dc.contributor.alternativeName조수현-
dc.contributor.alternativeName이지현-
dc.contributor.alternativeName구자일-
dc.contributor.alternativeName이성윤-
dc.contributor.alternativeNameBoovanahalli-
dc.contributor.alternativeName여석균-
dc.contributor.alternativeName이성준-
dc.contributor.alternativeName김영국-
dc.contributor.alternativeName김동희-
dc.contributor.alternativeName최용석-
dc.contributor.alternativeName송규용-
dc.identifier.bibliographicCitationEuropean Journal of Medicinal Chemistry, vol. 62, pp. 515-525-
dc.identifier.doi10.1016/j.ejmech.2013.01.020-
dc.subject.keywordACAT inhibitors-
dc.subject.keywordCellular cholesterol-
dc.subject.keywordLDL-
dc.subject.keywordNaphthoquinones-
dc.subject.keywordTriglycerides-
dc.subject.keywordVLDL-
dc.subject.localACAT inhibitor-
dc.subject.localACAT inhibitors-
dc.subject.localCellular cholesterol-
dc.subject.localLDL-
dc.subject.localNaphthoquinones-
dc.subject.localtriglyceride-
dc.subject.localTriglycerides-
dc.subject.localTriglyceride-
dc.subject.localtriglyceride (TG)-
dc.subject.localVLDL-
dc.description.journalClassY-
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