Property-Based Optimization of Hydroxamate-Based gamma-Lactam HDAC Inhibitors to Improve Their Metabolic Stability and Pharmacokinetic Profiles
DC Field | Value | Language |
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dc.contributor.author | Choi, Eunhyun | - |
dc.contributor.author | Lee, Chulho | - |
dc.contributor.author | Cho, Misun | - |
dc.contributor.author | Seo, Jeong Jea | - |
dc.contributor.author | Yang, Jee Sun | - |
dc.contributor.author | Oh, Soo Jin | - |
dc.contributor.author | Lee, Kiho | - |
dc.contributor.author | Park, Song-Kyu | - |
dc.contributor.author | Kim, Hwan Mook | - |
dc.contributor.author | Kwon, Ho Jeong | - |
dc.contributor.author | Han, Gyoonhee | - |
dc.date.accessioned | 2021-09-06T11:58:23Z | - |
dc.date.available | 2021-09-06T11:58:23Z | - |
dc.date.created | 2021-06-14 | - |
dc.date.issued | 2012-12-13 | - |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/106661 | - |
dc.description.abstract | Hydroxamate-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 gamma-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 gamma-lactam HDAC inhibitors were evaluated; the compound designated 8f had potent anticancer activity and high oral bioavailability. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | AMER CHEMICAL SOC | - |
dc.subject | HISTONE DEACETYLASE INHIBITORS | - |
dc.subject | THERAPY | - |
dc.subject | GROWTH | - |
dc.subject | BREAST | - |
dc.title | Property-Based Optimization of Hydroxamate-Based gamma-Lactam HDAC Inhibitors to Improve Their Metabolic Stability and Pharmacokinetic Profiles | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Lee, Kiho | - |
dc.contributor.affiliatedAuthor | Park, Song-Kyu | - |
dc.identifier.doi | 10.1021/jm3009376 | - |
dc.identifier.scopusid | 2-s2.0-84870986026 | - |
dc.identifier.wosid | 000312227300039 | - |
dc.identifier.bibliographicCitation | JOURNAL OF MEDICINAL CHEMISTRY, v.55, no.23, pp.10766 - 10770 | - |
dc.relation.isPartOf | JOURNAL OF MEDICINAL CHEMISTRY | - |
dc.citation.title | JOURNAL OF MEDICINAL CHEMISTRY | - |
dc.citation.volume | 55 | - |
dc.citation.number | 23 | - |
dc.citation.startPage | 10766 | - |
dc.citation.endPage | 10770 | - |
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.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.subject.keywordPlus | HISTONE DEACETYLASE INHIBITORS | - |
dc.subject.keywordPlus | THERAPY | - |
dc.subject.keywordPlus | GROWTH | - |
dc.subject.keywordPlus | BREAST | - |
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