dc.contributor.author | Bora-Tatar, Gamze | |
dc.contributor.author | Dayangac-Erden, Didem | |
dc.contributor.author | Demir, Ayhan S. | |
dc.contributor.author | Dalkara, Sevim | |
dc.contributor.author | Yelekçi, Kemal | |
dc.contributor.author | Erdem-Yurter, Hayat | |
dc.date.accessioned | 2019-06-27T08:05:37Z | |
dc.date.available | 2019-06-27T08:05:37Z | |
dc.date.issued | 2009 | |
dc.identifier.issn | 0968-0896 | en_US |
dc.identifier.issn | 1464-3391 | en_US |
dc.identifier.uri | https://hdl.handle.net/20.500.12469/1096 | |
dc.identifier.uri | https://doi.org/10.1016/j.bmc.2009.05.042 | |
dc.description.abstract | In 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. | en_US] |
dc.language.iso | eng | en_US |
dc.publisher | Pergamon-Elsevier Science Ltd | en_US |
dc.rights | info:eu-repo/semantics/openAccess | en_US |
dc.subject | HDAC inhibitors | en_US |
dc.subject | Molecular docking | en_US |
dc.subject | Caffeic acid derivatives | en_US |
dc.subject | Chlorogenic acid | en_US |
dc.subject | Curcumin | en_US |
dc.subject | Carboxylic acid derivatives | en_US |
dc.title | Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies | en_US |
dc.type | article | en_US |
dc.identifier.startpage | 5219 | en_US |
dc.identifier.endpage | 5228 | |
dc.relation.journal | Bioorganic & Medicinal Chemistry | en_US |
dc.identifier.issue | 14 | |
dc.identifier.volume | 17 | en_US |
dc.department | Fakülteler, Mühendislik ve Doğa Bilimleri Fakültesi, Biyoinformatik ve Genetik Bölümü | en_US |
dc.identifier.wos | WOS:000267873000044 | en_US |
dc.identifier.doi | 10.1016/j.bmc.2009.05.042 | en_US |
dc.identifier.scopus | 2-s2.0-67650078931 | en_US |
dc.institutionauthor | Yelekçi, Kemal | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |
dc.identifier.pmid | 19520580 | en_US |