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dc.contributor.authorŞahin, Zafer
dc.contributor.authorErtaş, Merve
dc.contributor.authorBerk, Barkın
dc.contributor.authorBiltekin, Sevde Nur
dc.contributor.authorYurttaş, Leyla
dc.contributor.authorDemirayak, Şeref
dc.date.accessioned10.07.201910:49:13
dc.date.accessioned2019-07-10T19:50:36Z
dc.date.available10.07.201910:49:13
dc.date.available2019-07-10T19:50:36Z
dc.date.issued2018en_US
dc.identifier.citationŞahin, Z., Ertaş, M., Berk, B., Biltekin, S., Yurttaş, L. ve Demirayak, Ş. (2018). Studies on non-steroidal inhibitors of aromatase enzyme; 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl)thiazole derivatives. Bioorganic & Medicinal Chemistry, 26(8), 1986-1995. https://dx.doi.org/10.1016/j.bmc.2018.02.048en_US
dc.identifier.issn0968-0896
dc.identifier.issn1464-3391
dc.identifier.urihttps://dx.doi.org/10.1016/j.bmc.2018.02.048
dc.identifier.urihttps://hdl.handle.net/20.500.12511/2030
dc.descriptionWOS: 000429533300056en_US
dc.descriptionPubMed ID: 29525337en_US
dc.description.abstractSteroidal and non-steroidal aromatase inhibitors target the suppression of estrogen biosynthesis in the treatment of breast cancer. Researchers have increasingly focused on developing non-steroidal derivatives for their potential clinical use avoiding steroidal side-effects. Non-steroidal derivatives generally have planar aromatic structures attached to the azole ring system. One part of this ring system comprises functional groups that inhibit aromatization through the coordination of the haem group of the aromatase enzyme. Replacement of the triazole ring system and development of aromatic/cyclic structures of the side chain can increase selectivity over aromatase enzyme inhibition. In this study, 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl) thiazole derivatives were synthesized and physical analyses and structural determination studies were performed. The IC50 values were determined by a fluorescence-based aromatase inhibition assay and compound 1 (4-(2-hydroxyphenyl)-2-(pyrimidine-2-yl) thiazole) were found potent inhibitor of enzyme (IC50: 0.42 nM). Then, their antiproliferative activity over MCF-7 and HEK-293 cell lines was evaluated using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Compounds 1, 7, 8, 13, 15, 18, 21 were active against MCF-7 breast cancer cells. Lastly, a series of docking experiments were undertaken to analyze the crystal structure of human placental aromatase and identify the possible interactions between the most active structure and the active site.en_US
dc.description.sponsorshipScientific and Technological Research Council of Turkey (TUBITAK) [SBAG-115S168]en_US
dc.description.sponsorshipThe authors acknowledge The Scientific and Technological Research Council of Turkey TUBITAK) for their financial support for the project SBAG-115S168.en_US
dc.language.isoengen_US
dc.publisherPergamon-Elsevier Science Ltden_US
dc.rightsinfo:eu-repo/semantics/embargoedAccessen_US
dc.subjectAnticanceren_US
dc.subjectMolecular Modellingen_US
dc.subjectThiazolesen_US
dc.subjectAromataseen_US
dc.subjectNon-Steroidalen_US
dc.titleStudies on non-steroidal inhibitors of aromatase enzyme; 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl)thiazole derivativesen_US
dc.typearticleen_US
dc.relation.ispartofBioorganic & Medicinal Chemistryen_US
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalıen_US
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Temel Eczacılık Bilimleri Bölümü, Farmasötik Mikrobiyoloji Ana Bilim Dalıen_US
dc.authorid0000-0001-6047-2796en_US
dc.authorid0000-0002-2289-7950en_US
dc.authorid0000-0001-6047-2796en_US
dc.authorid0000-0003-1896-2729en_US
dc.authorid0000-0002-0841-1299en_US
dc.identifier.volume26en_US
dc.identifier.issue8en_US
dc.identifier.startpage1986en_US
dc.identifier.endpage1995en_US
dc.relation.ecinfo:eu-repo/grantAgreement/TUBITAK/SOBAG/SBAG-115S168en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.identifier.doi10.1016/j.bmc.2018.02.048en_US
dc.identifier.wosqualityQ2en_US
dc.identifier.scopusqualityQ1en_US


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