Synthesis, bioevaluation and docking study of 5-substitutedphenyl-1,3,4-thiadiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents

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dc.contributor.authorN H Nam-
dc.contributor.authorT L Huong-
dc.contributor.authorD T M Dung-
dc.contributor.authorP T P Dung-
dc.contributor.authorD T K Oanh-
dc.contributor.authorS H Park-
dc.contributor.authorK Kim-
dc.contributor.authorB W Han-
dc.contributor.authorJi Eun Yun-
dc.contributor.authorJong Soon Kang-
dc.contributor.authorY Kim-
dc.contributor.authorS B Han-
dc.date.accessioned2017-04-19T09:55:54Z-
dc.date.available2017-04-19T09:55:54Z-
dc.date.issued2014-
dc.identifier.issn1475-6366-
dc.identifier.uri10.3109/14756366.2013.832238ko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/12159-
dc.description.abstractSince the first histone deacetylase (HDAC) inhibitor (Zolinza®, widely known as suberoylanilide hydroxamic acid; SAHA) was approved by the Food and Drug Administration for the treatment of T-cell lymphoma in 2006, the search for newer HDAC inhibitors has attracted a great deal of interest of medicinal chemists worldwide. As a continuity of our ongoing research in this area, we designed and synthesized a series of 5-substitutedphenyl-1,3,4-thiadiazole-based hydroxamic acids as analogues of SAHA and evaluated their biological activities. A number of compounds in this series, for example, N1-hydroxy-N8-(5-(2-chlorophenyl)-1,3,4-thiadiazol-2-yl)octandiamide (5b), N1-hydroxy-N8-(5-(3-chlorophenyl-1,3,4-thiadiazol-2-yl)octandiamide (5c) and N1-hydroxy-N8-(5-(4-chlorophenyl)-1,3,4-thiadiazol-2-yl)octandiamide (5d), were found to possess potent anticancer cytotoxicity and HDAC inhibition effects. Compounds 5b-d were generally two- to five-fold more potent in terms of cytotoxicity compared to SAHA against five cancer cell lines tested. Docking studies revealed that these hydroxamic acid displayed higher affinities than SAHA toward HDAC8-
dc.publisherT&F (Taylor & Francis)-
dc.titleSynthesis, bioevaluation and docking study of 5-substitutedphenyl-1,3,4-thiadiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents-
dc.title.alternativeSynthesis, bioevaluation and docking study of 5-substitutedphenyl-1,3,4-thiadiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents-
dc.typeArticle-
dc.citation.titleJournal of Enzyme Inhibition and Medicinal Chemistry-
dc.citation.number5-
dc.citation.endPage618-
dc.citation.startPage611-
dc.citation.volume29-
dc.contributor.affiliatedAuthorJi Eun Yun-
dc.contributor.affiliatedAuthorJong Soon Kang-
dc.contributor.alternativeNameNam-
dc.contributor.alternativeNameHuong-
dc.contributor.alternativeNameDung-
dc.contributor.alternativeNameDung-
dc.contributor.alternativeNameOanh-
dc.contributor.alternativeName박상호-
dc.contributor.alternativeName김경록-
dc.contributor.alternativeName한병우-
dc.contributor.alternativeName윤지은-
dc.contributor.alternativeName강종순-
dc.contributor.alternativeName김영수-
dc.contributor.alternativeName한상배-
dc.identifier.bibliographicCitationJournal of Enzyme Inhibition and Medicinal Chemistry, vol. 29, no. 5, pp. 611-618-
dc.identifier.doi10.3109/14756366.2013.832238-
dc.subject.keyword5-phenyl-1,3,4-thiadiazole-
dc.subject.keywordCytotoxicity-
dc.subject.keywordHeterocycle-
dc.subject.keywordHistone deacetylase (HDAC) inhibitors-
dc.subject.local5-phenyl-1,3,4-thiadiazole-
dc.subject.localCytotoxicity-
dc.subject.localcytotoxicity-
dc.subject.localheterocycles-
dc.subject.localHeterocycle-
dc.subject.localHistone deacetylase (HDAC) inhibitors-
dc.subject.localhistone deacetylase (HDAC) inhibitors-
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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