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Synthesis, bioevaluation and docking study of 5-substitutedphenyl-1,3,4-thiadiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents
DC Field | Value | Language |
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dc.contributor.author | Nam, Nguyen-Hai | - |
dc.contributor.author | Huong, Tran Lan | - |
dc.contributor.author | Dung, Do Thi Mai | - |
dc.contributor.author | Dung, Phan Thi Phuong | - |
dc.contributor.author | Oanh, Dao Thi Kim | - |
dc.contributor.author | Park, Sang Ho | - |
dc.contributor.author | Kim, Kyungrok | - |
dc.contributor.author | Han, Byung Woo | - |
dc.contributor.author | Yun, Jieun | - |
dc.contributor.author | Kang, Jong Soon | - |
dc.contributor.author | Kim, Youngsoo | - |
dc.contributor.author | Han, Sang-Bae | - |
dc.date.accessioned | 2023-04-20T01:14:33Z | - |
dc.date.available | 2023-04-20T01:14:33Z | - |
dc.date.created | 2017-11-15 | - |
dc.date.issued | 2014-10 | - |
dc.identifier.citation | Journal of Enzyme Inhibition and Medicinal Chemistry, Vol.29 No.5, pp.611-618 | - |
dc.identifier.issn | 1475-6366 | - |
dc.identifier.uri | https://hdl.handle.net/10371/191300 | - |
dc.description.abstract | Since the first histone deacetylase (HDAC) inhibitor (Zolinza (R), 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, N-1-hydroxy-N (8)-(5-(2-chlorophenyl)-1,3,4-thiadiazol-2-yl)octandiamide (5b), N-1-hydroxy-N-8-(5-(3-chlorophenyl-1,3,4-thiadiazol-2-yl)octandiamide (5c) and N-1-hydroxy-N-8-(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.language | 영어 | - |
dc.publisher | Taylor & Francis | - |
dc.title | Synthesis, bioevaluation and docking study of 5-substitutedphenyl-1,3,4-thiadiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents | - |
dc.type | Article | - |
dc.identifier.doi | 10.3109/14756366.2013.832238 | - |
dc.citation.journaltitle | Journal of Enzyme Inhibition and Medicinal Chemistry | - |
dc.identifier.wosid | 000342056900001 | - |
dc.identifier.scopusid | 2-s2.0-84907063089 | - |
dc.citation.endpage | 618 | - |
dc.citation.number | 5 | - |
dc.citation.startpage | 611 | - |
dc.citation.volume | 29 | - |
dc.description.isOpenAccess | Y | - |
dc.contributor.affiliatedAuthor | Han, Byung Woo | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.subject.keywordPlus | HDAC INHIBITORS | - |
dc.subject.keywordPlus | CANCER | - |
dc.subject.keywordPlus | UPDATE | - |
dc.subject.keywordAuthor | 5-phenyl-1,3,4-thiadiazole | - |
dc.subject.keywordAuthor | cytotoxicity | - |
dc.subject.keywordAuthor | heterocycle | - |
dc.subject.keywordAuthor | histone deacetylase (HDAC) inhibitors | - |
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