Structure and property based design, synthesis and biological evaluation of gamma-lactam based HDAC inhibitors: Part II
DC Field | Value | Language |
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dc.contributor.author | Lee, Chulho | - |
dc.contributor.author | Choi, Eunhyun | - |
dc.contributor.author | Cho, Misun | - |
dc.contributor.author | Lee, Boah | - |
dc.contributor.author | Oh, Soo Jin | - |
dc.contributor.author | Park, Song-Kyu | - |
dc.contributor.author | Lee, Kiho | - |
dc.contributor.author | Kim, Hwan Mook | - |
dc.contributor.author | Han, Gyoonhee | - |
dc.date.accessioned | 2021-09-06T18:41:10Z | - |
dc.date.available | 2021-09-06T18:41:10Z | - |
dc.date.created | 2021-06-18 | - |
dc.date.issued | 2012-06-15 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/108153 | - |
dc.description.abstract | Histone deacetylases (HDACs) are involved in post-translational modification and epi-genetic expression, and have been the intriguing targets for treatment of cancer. In previous study, we reported synthesis and the biological preliminary results of gamma-lactam based HDAC inhibitors. Based on the previous results, smaller gamma-lactam core HDAC inhibitors are more active than the corresponding series of larger delta-lactam based analogues and the hydrophobic and bulky cap groups are required for better potency which decreased microsomal stability. Thus, gamma-lactam analogues with methoxy, trifluoromethyl groups of ortho-, meta-, para-positions of cap group were prepared and evaluated their biological potency. Among them, trifluoromethyl analogues, which have larger lipophilicity, showed better HDAC inhibitory activity than other analogues. In overall, lipophilicity leads to increase hydrophobic interaction between surface of HDAC active site and HDAC inhibitor, improves HDAC inhibitory activity. (C) 2012 Elsevier Ltd. All rights reserved. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.subject | HISTONE DEACETYLASE | - |
dc.subject | THERAPY | - |
dc.title | Structure and property based design, synthesis and biological evaluation of gamma-lactam based HDAC inhibitors: Part II | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Park, Song-Kyu | - |
dc.contributor.affiliatedAuthor | Lee, Kiho | - |
dc.identifier.doi | 10.1016/j.bmcl.2012.04.045 | - |
dc.identifier.scopusid | 2-s2.0-84861571256 | - |
dc.identifier.wosid | 000304484600069 | - |
dc.identifier.bibliographicCitation | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.22, no.12, pp.4189 - 4192 | - |
dc.relation.isPartOf | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.citation.title | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.citation.volume | 22 | - |
dc.citation.number | 12 | - |
dc.citation.startPage | 4189 | - |
dc.citation.endPage | 4192 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
dc.subject.keywordPlus | HISTONE DEACETYLASE | - |
dc.subject.keywordPlus | THERAPY | - |
dc.subject.keywordAuthor | Histone deacetylases | - |
dc.subject.keywordAuthor | Inhibitor | - |
dc.subject.keywordAuthor | Docking | - |
dc.subject.keywordAuthor | Property | - |
dc.subject.keywordAuthor | Optimization | - |
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