Modification of cap group in δ-lactam-based histone deacetylase (HDAC) inhibitors

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dc.contributor.authorHwan Mook Kim-
dc.contributor.authorS H Hong-
dc.contributor.authorM S Kim-
dc.contributor.authorChang Woo Lee-
dc.contributor.authorJong Soon Kang-
dc.contributor.authorKiho Lee-
dc.contributor.authorSong Kyu Park-
dc.contributor.authorJ W Han-
dc.contributor.authorH Y Lee-
dc.contributor.authorY Choi-
dc.contributor.authorH J Kwon-
dc.contributor.authorG Han-
dc.date.accessioned2017-04-19T09:08:22Z-
dc.date.available2017-04-19T09:08:22Z-
dc.date.issued2007-
dc.identifier.issn0960-894X-
dc.identifier.uri10.1016/j.bmcl.2007.09.034ko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/8140-
dc.description.abstractNovel δ-lactam-based HDAC inhibitors which have various substituted benzyl, bi-aromatic cap groups were prepared using ring closure metathesis reaction, and evaluated their HDAC inhibitory activities and anti-proliferative effects. Among prepared analogues, 11m and 11o have very strong HDAC enzymatic inhibition and showed the most potent growth inhibitory activity to five human tumor cell lines including PC-3, ACHN, NUGC-3, HCT-15, and MBA-MB-231 tumor cell lines. Compounds 11m and 11o also showed good tumor growth inhibition of MDA-MB-231 cells in in vivo xenograft model. Structure-activity relationship study using docking model explained the significance of hydrophobic aromatic cap groups for their in vitro activities.-
dc.publisherElsevier-
dc.titleModification of cap group in δ-lactam-based histone deacetylase (HDAC) inhibitors-
dc.title.alternativeModification of cap group in δ-lactam-based histone deacetylase (HDAC) inhibitors-
dc.typeArticle-
dc.citation.titleBioorganic & Medicinal Chemistry Letters-
dc.citation.number22-
dc.citation.endPage6238-
dc.citation.startPage6234-
dc.citation.volume17-
dc.contributor.affiliatedAuthorHwan Mook Kim-
dc.contributor.affiliatedAuthorChang Woo Lee-
dc.contributor.affiliatedAuthorJong Soon Kang-
dc.contributor.affiliatedAuthorKiho Lee-
dc.contributor.affiliatedAuthorSong Kyu Park-
dc.contributor.alternativeName김환묵-
dc.contributor.alternativeName홍성희-
dc.contributor.alternativeName김명숙-
dc.contributor.alternativeName이창우-
dc.contributor.alternativeName강종순-
dc.contributor.alternativeName이기호-
dc.contributor.alternativeName박성규-
dc.contributor.alternativeName한정환-
dc.contributor.alternativeName이희윤-
dc.contributor.alternativeName최용석-
dc.contributor.alternativeName권호정-
dc.contributor.alternativeName한균희-
dc.identifier.bibliographicCitationBioorganic & Medicinal Chemistry Letters, vol. 17, no. 22, pp. 6234-6238-
dc.identifier.doi10.1016/j.bmcl.2007.09.034-
dc.subject.keywordAnticancer chemotherapy-
dc.subject.keywordDocking model-
dc.subject.keywordEnzyme inhibitor-
dc.subject.keywordGrowth inhibition-
dc.subject.keywordHDAC-
dc.subject.keywordHistone deacetylase-
dc.subject.keywordIn vivo xenograft model-
dc.subject.localAnticancer chemotherapy-
dc.subject.localDocking model-
dc.subject.localEnzyme inhibitor-
dc.subject.localenzyme inhibitors-
dc.subject.localGrowth Inhibition-
dc.subject.localgrowth inhibition-
dc.subject.localGrowth inhibition-
dc.subject.localHDAC-
dc.subject.localHistone deacetylase-
dc.subject.localhistone deacetylase (HDAC)-
dc.subject.localHistone deacetylases-
dc.subject.localhistone deacetylase-
dc.subject.localIn vivo xenograft model-
dc.description.journalClassY-
Appears in Collections:
Ochang Branch Institute > Division of National Bio-Infrastructure > Laboratory Animal Resource & Research Center > 1. Journal Articles
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