Synthesis of a radioiodinated antiestrogen glucuronide compound (TAM-G)

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dc.contributor.authorMuftuler, Fazilet Zumrut Biber
dc.contributor.authorUnak, Perihan
dc.contributor.authorIchedef, Cigdem
dc.contributor.authorDemir, Ilknur
dc.date.accessioned2019-10-27T21:24:57Z
dc.date.available2019-10-27T21:24:57Z
dc.date.issued2011
dc.departmentEge Üniversitesien_US
dc.description.abstractTamoxifen [TAM; ([Z]-2-[4-(1,2-diphenyl-1-di-butenyl)-phenoxy]-N,N-dimethylethanamine) has been used as an antiestrogen drug for treatment and prevention of human breast cancer. The aim of this study is conjugation of hydrophilic glucuronic acid to the starting substance TAM and labeling with I-131 using iodogen as oxidizing agent. The reactions are completed in three steps, including enzymatic reaction, with the following sub-steps; preparation of microsomal fraction from rat liver and subsequent purification of UDP-glucuronyl transferase (UDPGT), estimation of protein amount in microsomal samples and glucuronidation reaction. Synthesized glucuronide derivative (TAM-G) was purified using high performance liquid chromatography (HPLC). Mass spectroscopy of cold standard showed that the labeling most probably occurs in ortho position to the aromatic ring containing the ether group of TAM-G as expected. Radiochemical yield of the I-131 labeled TAM-G ([I-131]TAM-G) is determined by using Thin Layer Radio Chromatography (TLRC). The radiopharmaceutical potential of [I-131]TAM-G is examined by biodistribution studies that is run on normal female Albino Wistar rats. According to biodistribution results I-131 labeled TAM-G may be proposed as a new antiestrogen glucuronide imaging agent for breast and uterus.en_US
dc.description.sponsorshipT.R. Prime Ministry State Planning Organization [06 DPT 06]; Ege UniversityEge University [2007 NBE 006]en_US
dc.description.sponsorshipThis work financially supported by T.R. Prime Ministry State Planning Organization Contract No 06 DPT 06 and Ege University Research Fund contact no 2007 NBE 006.en_US
dc.identifier.doi10.1007/s10967-010-0932-7
dc.identifier.endpage689en_US
dc.identifier.issn0236-5731
dc.identifier.issn1588-2780
dc.identifier.issn0236-5731en_US
dc.identifier.issn1588-2780en_US
dc.identifier.issue3en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.startpage679en_US
dc.identifier.urihttps://doi.org/10.1007/s10967-010-0932-7
dc.identifier.urihttps://hdl.handle.net/11454/44709
dc.identifier.volume287en_US
dc.identifier.wosWOS:000287756900002en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherSpringeren_US
dc.relation.ispartofJournal of Radioanalytical and Nuclear Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectTamoxifen (TAM)en_US
dc.subject[I-131]en_US
dc.subjectAntiestrogenen_US
dc.subject[I-131] Labeled Tamoxifen-glucuronide ([I-131]TAM-G)en_US
dc.titleSynthesis of a radioiodinated antiestrogen glucuronide compound (TAM-G)en_US
dc.typeArticleen_US

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