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Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling
dc.creator | Bouchet, Samuel | |
dc.creator | Linot, Camille | |
dc.creator | Ružić, Dušan | |
dc.creator | Agbaba, Danica | |
dc.creator | Fouchaq, Benoit | |
dc.creator | Roche, Joelle | |
dc.creator | Nikolić, Katarina | |
dc.creator | Blanquart, Christophe | |
dc.creator | Bertrand, Philippe | |
dc.date.accessioned | 2019-09-02T12:11:29Z | |
dc.date.available | 2019-09-02T12:11:29Z | |
dc.date.issued | 2019 | |
dc.identifier.issn | 1948-5875 | |
dc.identifier.uri | https://farfar.pharmacy.bg.ac.rs/handle/123456789/3354 | |
dc.description.abstract | Dissymmetric cross metathesis of alkenes as a convergent and general synthetic strategy allowed for the preparation of a new small series of human histone deacetylases (HDAC) inhibitors. Alkenes bearing Bocprotected hydroxamic acid and benzamide and trityl-protected thiols were used to provide the zinc binding groups and were reacted with alkenes bearing aromatic cap groups. One compound was identified as a selective HDAC6 inhibitor lead. Additional biological evaluation in cancer cell lines demonstrated its ability to stimulate the expression of the epithelial marker E-cadherin and tumor suppressor genes like SEMA3F and p21, suggesting a potential use of this compound for lung cancer treatment. Molecular docking on all 11 HDAC isoforms was used to rationalize the observed biological results. | en |
dc.publisher | Amer Chemical Soc, Washington | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172033/RS// | |
dc.rights | restrictedAccess | |
dc.source | ACS Medicinal Chemistry Letters | |
dc.subject | Cross metathesis | en |
dc.subject | histone deacetylases | en |
dc.subject | lung cancer | en |
dc.subject | epigenetics | en |
dc.subject | molecular modeling | en |
dc.title | Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling | en |
dc.type | article | |
dc.rights.license | ARR | |
dcterms.abstract | Линот, Цамилле; Боуцхет, Самуел; Николић, Катарина; Ружић, Душан; Aгбаба, Даница; Фоуцхаq, Беноит; Роцхе, Јоелле; Бланqуарт, Цхристопхе; Бертранд, Пхилиппе; | |
dc.citation.volume | 10 | |
dc.citation.issue | 6 | |
dc.citation.spage | 863 | |
dc.citation.epage | 868 | |
dc.citation.other | 10(6): 863-868 | |
dc.citation.rank | M21 | |
dc.identifier.wos | 000471834600006 | |
dc.identifier.doi | 10.1021/acsmedchemlett.8b00440 | |
dc.identifier.pmid | 31223439 | |
dc.identifier.scopus | 2-s2.0-85066886661 | |
dc.type.version | publishedVersion |