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

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dc.contributor.authorKim, HMko
dc.contributor.authorHong, SHko
dc.contributor.authorKim, MSko
dc.contributor.authorLee, CWko
dc.contributor.authorKang, JSko
dc.contributor.authorLee, Kko
dc.contributor.authorPark, SKko
dc.contributor.authorHan, JWko
dc.contributor.authorLee, Hee Yoonko
dc.contributor.authorChoi, Yko
dc.contributor.authorKwon, HJko
dc.contributor.authorHan, Gko
dc.date.accessioned2013-03-07T08:50:52Z-
dc.date.available2013-03-07T08:50:52Z-
dc.date.created2012-02-06-
dc.date.created2012-02-06-
dc.date.issued2007-11-
dc.identifier.citationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.17, no.72, pp.6234 - 6238-
dc.identifier.issn0960-894X-
dc.identifier.urihttp://hdl.handle.net/10203/89826-
dc.description.abstractNovel delta-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. (C) 2007 Elsevier Ltd. All rights reserved.-
dc.languageEnglish-
dc.publisherPERGAMON-ELSEVIER SCIENCE LTD-
dc.subjectPROLIFERATION-
dc.subjectGROWTH-
dc.subjectCELLS-
dc.titleModification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors-
dc.typeArticle-
dc.identifier.wosid000250906200039-
dc.identifier.scopusid2-s2.0-35148888600-
dc.type.rimsART-
dc.citation.volume17-
dc.citation.issue72-
dc.citation.beginningpage6234-
dc.citation.endingpage6238-
dc.citation.publicationnameBIOORGANIC & MEDICINAL CHEMISTRY LETTERS-
dc.identifier.doi10.1016/j.bmcl.2007.09.034-
dc.contributor.localauthorLee, Hee Yoon-
dc.contributor.nonIdAuthorKim, HM-
dc.contributor.nonIdAuthorHong, SH-
dc.contributor.nonIdAuthorKim, MS-
dc.contributor.nonIdAuthorLee, CW-
dc.contributor.nonIdAuthorKang, JS-
dc.contributor.nonIdAuthorLee, K-
dc.contributor.nonIdAuthorPark, SK-
dc.contributor.nonIdAuthorHan, JW-
dc.contributor.nonIdAuthorChoi, Y-
dc.contributor.nonIdAuthorKwon, HJ-
dc.contributor.nonIdAuthorHan, G-
dc.type.journalArticleArticle-
dc.subject.keywordAuthorhistone deacetylase-
dc.subject.keywordAuthorHDAC-
dc.subject.keywordAuthoranticancer chemotherapy-
dc.subject.keywordAuthorenzyme inhibitor-
dc.subject.keywordAuthorgrowth inhibition-
dc.subject.keywordAuthorin vivo xenograft model-
dc.subject.keywordAuthordocking model-
dc.subject.keywordPlusPROLIFERATION-
dc.subject.keywordPlusGROWTH-
dc.subject.keywordPlusCELLS-
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