Structure and property based design, synthesis and biological evaluation of gamma-lactam based HDAC inhibitors

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dc.contributor.authorE Choi-
dc.contributor.authorC Lee-
dc.contributor.authorJ E Park-
dc.contributor.authorJ J Seo-
dc.contributor.authorM Cho-
dc.contributor.authorJong Soon Kang-
dc.contributor.authorHwan Mook Kim-
dc.contributor.authorSong Kyu Park-
dc.contributor.authorKiho Lee-
dc.contributor.authorG Han-
dc.date.accessioned2017-04-19T09:21:29Z-
dc.date.available2017-04-19T09:21:29Z-
dc.date.issued2011-
dc.identifier.issn0960894X-
dc.identifier.uri10.1016/j.bmcl.2010.12.079ko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/9984-
dc.description.abstractHistone deacetylases (HDACs) are involved in post-translational modification and gene expression. Cancer cells recruited amounts of HDACs for their survival by epi-genetic down regulation of tumor suppressor genes. HDACs have been the promising targets for treatment of cancer, and many HDAC inhibitors have been investigated nowadays. In previous study, we synthesized δ-lactam core HDAC inhibitors which showed potent HDAC inhibitory activities as well as cancer cell growth inhibitory activities. Through QSAR study of the δ-lactam based inhibitors, the smaller core is suggested as more active than larger one because it fits better in narrow hydrophobic tunnel of the active pocket of HDAC enzyme. The smaller γ-lactam core HDAC inhibitors were designed and synthesized for biological and property optimization. Phenyl, naphthyl and thiophenyl groups were introduced as the cap groups. Hydrophobic and bulky cap groups increase potency of HDAC inhibition because of hydrophobic interaction between HDAC and inhibitors. In overall, γ-lactam based HDAC inhibitors showed more potent than δ-lactam analogues.-
dc.publisherElsevier-
dc.titleStructure and property based design, synthesis and biological evaluation of gamma-lactam based HDAC inhibitors-
dc.title.alternativeStructure and property based design, synthesis and biological evaluation of gamma-lactam based HDAC inhibitors-
dc.typeArticle-
dc.citation.titleBioorganic & Medicinal Chemistry Letters-
dc.citation.number4-
dc.citation.endPage1221-
dc.citation.startPage1218-
dc.citation.volume21-
dc.contributor.affiliatedAuthorJong Soon Kang-
dc.contributor.alternativeName최은현-
dc.contributor.alternativeName이철호-
dc.contributor.alternativeName박정은-
dc.contributor.alternativeName서정재-
dc.contributor.alternativeName조미선-
dc.contributor.alternativeName강종순-
dc.contributor.alternativeName김환묵-
dc.contributor.alternativeName박성규-
dc.contributor.alternativeName이기호-
dc.contributor.alternativeName한균희-
dc.identifier.bibliographicCitationBioorganic & Medicinal Chemistry Letters, vol. 21, no. 4, pp. 1218-1221-
dc.identifier.doi10.1016/j.bmcl.2010.12.079-
dc.subject.keywordADME-
dc.subject.keywordAnticancer-
dc.subject.keywordDocking study-
dc.subject.keywordHDAC-
dc.subject.keywordHistone deacetylase-
dc.subject.keywordIn vitro activity-
dc.subject.keywordInhibitor-
dc.subject.keywordIsoform-
dc.subject.localADME-
dc.subject.localAnticancer-
dc.subject.localDocking study-
dc.subject.localHDAC-
dc.subject.localHistone deacetylase-
dc.subject.localIn vitro activity-
dc.subject.localInhibitor-
dc.subject.localIsoform-
dc.description.journalClassY-
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Ochang Branch Institute > Division of Bioinfrastructure > Laboratory Animal Resource Center > 1. Journal Articles
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