Property-based optimization of hydroxamate-based γ-lactam HDAC inhibitors to improve their metabolic stability and pharmacokinetic profiles

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dc.contributor.authorE Choi-
dc.contributor.authorC H Lee-
dc.contributor.authorM Cho-
dc.contributor.authorJ J Seo-
dc.contributor.authorJ S Yang-
dc.contributor.authorSoo Jin Oh-
dc.contributor.authorK Lee-
dc.contributor.authorS K Park-
dc.contributor.authorH M Kim-
dc.contributor.authorH J Kwon-
dc.contributor.authorG Han-
dc.date.accessioned2017-04-19T09:35:59Z-
dc.date.available2017-04-19T09:35:59Z-
dc.date.issued2012-
dc.identifier.issn0022-2623-
dc.identifier.uri10.1021/jm3009376ko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/11115-
dc.description.abstractHydroxamate-based HDAC inhibitors have promising anticancer activities but metabolic instability and poor pharmacokinetics leading to poor in vivo results. QSAR and PK studies of HDAC inhibitors showed that a γ-lactam core and a modified cap group, including halo, alkyl, and alkoxy groups with various carbon chain linkers, improved HDAC inhibition and metabolic stability. The biological properties of the γ-lactam HDAC inhibitors were evaluated; the compound designated 8f had potent anticancer activity and high oral bioavailability.-
dc.publisherAmer Chem Soc-
dc.titleProperty-based optimization of hydroxamate-based γ-lactam HDAC inhibitors to improve their metabolic stability and pharmacokinetic profiles-
dc.title.alternativeProperty-based optimization of hydroxamate-based γ-lactam HDAC inhibitors to improve their metabolic stability and pharmacokinetic profiles-
dc.typeArticle-
dc.citation.titleJournal of Medicinal Chemistry-
dc.citation.number23-
dc.citation.endPage10770-
dc.citation.startPage10766-
dc.citation.volume55-
dc.contributor.affiliatedAuthorSoo Jin Oh-
dc.contributor.alternativeName최은현-
dc.contributor.alternativeName이철호-
dc.contributor.alternativeName조미선-
dc.contributor.alternativeName서정재-
dc.contributor.alternativeName양지선-
dc.contributor.alternativeName오수진-
dc.contributor.alternativeName이기호-
dc.contributor.alternativeName박성규-
dc.contributor.alternativeName김환묵-
dc.contributor.alternativeName권호정-
dc.contributor.alternativeName한균희-
dc.identifier.bibliographicCitationJournal of Medicinal Chemistry, vol. 55, no. 23, pp. 10766-10770-
dc.identifier.doi10.1021/jm3009376-
dc.description.journalClassY-
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