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Ring-truncated deguelin derivatives as potent Hypoxia Inducible Factor-1α (HIF-1α) inhibitors : Ring-truncated deguelin derivatives as potent Hypoxia Inducible Factor-1 alpha (HIF-1 alpha) inhibitors
DC Field | Value | Language |
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dc.contributor.author | Kim, Ho Shin | - |
dc.contributor.author | Hong, Mannkyu | - |
dc.contributor.author | Lee, Su-Chan | - |
dc.contributor.author | Lee, Ho-Young | - |
dc.contributor.author | Suh, Young-Ger | - |
dc.contributor.author | Oh, Dong-Chan | - |
dc.contributor.author | Seo, Ji Hae | - |
dc.contributor.author | Choi, Hoon | - |
dc.contributor.author | Kim, Jun Yong | - |
dc.contributor.author | Kim, Kyu-Won | - |
dc.contributor.author | Kim, Jeong Hun | - |
dc.contributor.author | Kim, Joohwan | - |
dc.contributor.author | Kim, Young-Myeong | - |
dc.contributor.author | Park, So-Jung | - |
dc.contributor.author | Park, Hyun-Ju | - |
dc.contributor.author | Lee, Jeewoo | - |
dc.date.accessioned | 2024-08-08T01:38:29Z | - |
dc.date.available | 2024-08-08T01:38:29Z | - |
dc.date.created | 2017-11-15 | - |
dc.date.created | 2017-11-15 | - |
dc.date.issued | 2015-11 | - |
dc.identifier.citation | European Journal of Medicinal Chemistry, Vol.104, pp.157-164 | - |
dc.identifier.issn | 0223-5234 | - |
dc.identifier.uri | https://hdl.handle.net/10371/207102 | - |
dc.description.abstract | A series of fluorophenyl and pyridine analogues of 1 and 2 were synthesized as ring-truncated deguelin surrogates and evaluated for their HIF-1 alpha inhibition. Their structure-activity relationship was systematically investigated based on the variation of the linker B-region moiety. Among the inhibitors, compound 25 exhibited potent HIF-1 alpha inhibition in a dose-dependent manner and significant antitumor activity in H1299 with less toxicity than deguelin. It also inhibited in vitro hypoxia-mediated angiogenic processes in HRMECs. The docking study indicates that 25 occupied the C-terminal ATP-binding pocket of HSP90 in a similar mode as 1, which implies that the anticancer and antiangiogenic activities of 25 are derived from HIF-1 alpha destabilization by binding to the C-terminal ATP-binding site of hHSP90. (C) 2015 Elsevier Masson SAS. All rights reserved. | - |
dc.language | 영어 | - |
dc.publisher | Elsevier BV | - |
dc.title | Ring-truncated deguelin derivatives as potent Hypoxia Inducible Factor-1α (HIF-1α) inhibitors | - |
dc.title.alternative | Ring-truncated deguelin derivatives as potent Hypoxia Inducible Factor-1 alpha (HIF-1 alpha) inhibitors | - |
dc.type | Article | - |
dc.identifier.doi | 10.1016/j.ejmech.2015.09.033 | - |
dc.citation.journaltitle | European Journal of Medicinal Chemistry | - |
dc.identifier.wosid | 000363828000015 | - |
dc.identifier.scopusid | 2-s2.0-84945177144 | - |
dc.citation.endpage | 164 | - |
dc.citation.startpage | 157 | - |
dc.citation.volume | 104 | - |
dc.description.isOpenAccess | N | - |
dc.contributor.affiliatedAuthor | Lee, Ho-Young | - |
dc.contributor.affiliatedAuthor | Suh, Young-Ger | - |
dc.contributor.affiliatedAuthor | Oh, Dong-Chan | - |
dc.contributor.affiliatedAuthor | Kim, Jeong Hun | - |
dc.contributor.affiliatedAuthor | Lee, Jeewoo | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.subject.keywordPlus | C-TERMINAL DOMAIN | - |
dc.subject.keywordPlus | FACTOR 1-ALPHA | - |
dc.subject.keywordPlus | PROTEIN-KINASE | - |
dc.subject.keywordPlus | BINDING-SITE | - |
dc.subject.keywordPlus | ATP BINDING | - |
dc.subject.keywordPlus | HSP90 | - |
dc.subject.keywordPlus | CANCER | - |
dc.subject.keywordPlus | EXPRESSION | - |
dc.subject.keywordPlus | OVEREXPRESSION | - |
dc.subject.keywordPlus | PROLIFERATION | - |
dc.subject.keywordAuthor | Hypoxia Inducible Factor-1 | - |
dc.subject.keywordAuthor | HIF-1 | - |
dc.subject.keywordAuthor | Heat shock protein 90 | - |
dc.subject.keywordAuthor | HSP90 | - |
dc.subject.keywordAuthor | Antitumor | - |
dc.subject.keywordAuthor | Deguelin | - |
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