Synthesis and biological investigation of hydrogenated and fluorinated amino acid-based molecules that may bind specifically to the alpha 5/beta1 integrin
dc.contributor.advisor | Coşgun, Sedat | |
dc.contributor.advisor | Işık, Sevim | |
dc.contributor.author | Demir, Ayşe | |
dc.date.accessioned | 2021-05-07T11:39:40Z | |
dc.date.available | 2021-05-07T11:39:40Z | |
dc.date.submitted | 2010 | |
dc.date.issued | 2018-08-06 | |
dc.identifier.uri | https://acikbilim.yok.gov.tr/handle/20.500.12812/615978 | |
dc.description.abstract | İntegrinler hücre ? hücre adezyonunda ve hücre ? ekstraselüler matriks (ESM) adezyonunda rol alan hücre yüzeyi respestörleridirler ki aynı zamanda hücre göçünde ve hücre haberleşmesinde (signaling) yer alırlar. ?5ß1 integrinler beyin tumor hücrelerinde geniş bir yelpazede bulunur.Bu çalışmada, en spesifik ?5ß1 integrin antagonisti olan psödopeptit SJ749 molekülünün spiroizoksazolinopirol ara ürünü sentezlenmiştir. Fischer Esterleşme reaksiyonu, Swern oksidasyonu, ve Wittig olefinasyonu reaksiyonları uygulanmıştır. Bunun ardından SJ749'daki (2,4,6-trimetihylfenil)sülfonil alaninin olduğu yere kenetlenmek üzere florlu diaminopropiyonat molekülleri sentezlenmiştir. Son olarak da, sentezlenen moleküllerin biyolojik aktiviteleri gerçekleştirilmiştir. Bunlar, A-172 ve U-87 astrositoma hücre soylarında sitotoksisite, hücre proliferasyonu, ve sitotoksisite mevcutsa apoptoz deneyleridir. | |
dc.description.abstract | Integrins are cell surface receptors that take part in cell ? cell adhesion and cell ? extracellular matrix (ECM) adhesion events as well as in cell migration and cell signaling. ?5ß1 integrins are expressed on a wide range among brain tumor cells.In this study, an intermediate spiroisoxazolinopyrrole of the most specific ?5ß1 integrin antagonist SJ749 was synthesized. Fischer esterification reaction, Swern oxidation, and Wittig olefination were performed. Next, fluorinated diaminopropionate molecules were synthesized for coupling to SJ749 instead of the (2,4,6-trimethylphenyl) diaminopropionate. At the end, biological evaluation of the molecules synthesized was performed. These assays included cytotoxicity, and cell proliferation and apoptosis if cytotoxicity was observed. | en_US |
dc.language | English | |
dc.language.iso | en | |
dc.rights | info:eu-repo/semantics/openAccess | |
dc.rights | Attribution 4.0 United States | tr_TR |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0/ | |
dc.subject | Biyokimya | tr_TR |
dc.subject | Biochemistry | en_US |
dc.subject | Eczacılık ve Farmakoloji | tr_TR |
dc.subject | Pharmacy and Pharmacology | en_US |
dc.subject | Kimya | tr_TR |
dc.subject | Chemistry | en_US |
dc.title | Synthesis and biological investigation of hydrogenated and fluorinated amino acid-based molecules that may bind specifically to the alpha 5/beta1 integrin | |
dc.title.alternative | Alfa5/beta1 integrine bağlanması olası amino asit bazlı hidrojenli ve florlu moleküllerin sentezi ve biyolojik özelliklerinin incelenmesi | |
dc.type | masterThesis | |
dc.date.updated | 2018-08-06 | |
dc.contributor.department | Kimya Ana Bilim Dalı | |
dc.subject.ytm | In vitro | |
dc.subject.ytm | Integrins | |
dc.subject.ytm | Astrocytoma | |
dc.subject.ytm | Amino acids | |
dc.subject.ytm | Drugs | |
dc.subject.ytm | Drug evaluation | |
dc.subject.ytm | Alanine | |
dc.identifier.yokid | 385466 | |
dc.publisher.institute | Fen Bilimleri Enstitüsü | |
dc.publisher.university | FATİH ÜNİVERSİTESİ | |
dc.identifier.thesisid | 283707 | |
dc.description.pages | 98 | |
dc.publisher.discipline | Diğer |