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dc.contributor.authorBora-Tatar, Gamze
dc.contributor.authorDayangac-Erden, Didem
dc.contributor.authorDemir, Ayhan S.
dc.contributor.authorDalkara, Sevim
dc.contributor.authorYelekçi, Kemal
dc.contributor.authorErdem-Yurter, Hayat
dc.date.accessioned2019-06-27T08:05:37Z
dc.date.available2019-06-27T08:05:37Z
dc.date.issued2009
dc.identifier.issn0968-0896
dc.identifier.issn1464-3391
dc.identifier.urihttps://hdl.handle.net/20.500.12469/1096
dc.identifier.urihttps://doi.org/10.1016/j.bmc.2009.05.042
dc.description.abstractIn the light of known HDAC inhibitors 33 carboxylic acid derivatives were tested to understand the structural requirements for HDAC inhibition activity. Several modifications were applied to develop the structure-activity relationships of carboxylic acid HDAC inhibitors. HDAC inhibition activities were investigated in vitro by using HeLa nuclear extract in a fluorimetric assay. Molecular docking was also carried out for the human HDAC8 enzyme in order to predict inhibition activity and the 3D poses of inhibitor-enzyme complexes. Of these compounds caffeic acid derivatives such as chlorogenic acid and curcumin were found to be highly potent compared to sodium butyrate which is a well-known HDAC inhibitor. (C) 2009 Elsevier Ltd. All rights reserved.
dc.language.isoEnglish
dc.publisherPergamon-Elsevier Science Ltd
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectHDAC inhibitors
dc.subjectMolecular docking
dc.subjectCaffeic acid derivatives
dc.subjectChlorogenic acid
dc.subjectCurcumin
dc.subjectCarboxylic acid derivatives
dc.titleMolecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies
dc.typeArticle
dc.identifier.startpage5219
dc.identifier.endpage5228
dc.relation.journalBioorganic & Medicinal Chemistry
dc.identifier.issue14
dc.identifier.volume17
dc.identifier.wosWOS:000267873000044
dc.identifier.doi10.1016/j.bmc.2009.05.042
dc.contributor.khasauthorYelekçi, Kemal


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