Synthesis of an estradiol glucuronide derivative and investigation of its radiopharmaceutical potential

Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine
F Z BiberH Durak

Abstract

The aim of the current study was to synthesize a derivative of estradiol glucuronide, which is able to be labeled with 99mTc and to investigate its radiopharmaceutical potential using imaging and biodistribution studies. An estrogen derivative, beta-estradiol (1,3,5,[10]-estratriene-3,17beta-diol) attached to diethylenetriamine pentaacetic acid (DTPA) was synthesized in six steps. At the end of these steps a compound of estradiol and DTPA derivative called deoxy demethyl homoestradiolyl diethylenetriamine pentaacetic acid (ESTDTPA) was synthesized. Afterwards, this compound was reacted with UDP-glucuronyl transferase (UDPGT). Following the glucuronidation reaction, the product called deoxy demethyl homoestradiolyl diethylenetriamine pentaaceticacid-glucuronide (ESTDTPAG) was obtained. Synthesized products were purified using high performance liquid chromatography (HPLC). The identification of the purified products and impurities were also established using HPLC. Synthesized compound was labeled with 99mTc. Thin layer radio chromatography (TLRC) technique was used to determine their radiochemical yields and stabilities. Labeling yield was over 96%. The biodistribution studies were performed on female Albino Wistar rats. The acti...Continue Reading

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Citations

Jun 29, 2010·Cancer Biotherapy & Radiopharmaceuticals·Ilker Emin MedineFeriha Toksöz
Sep 29, 2011·Cancer Biotherapy & Radiopharmaceuticals·Serap TeksözMine Şencan Eren
May 17, 2008·Nuclear Medicine and Biology·Uğur AvcibaşiEbru Rükşen Dursun
Nov 27, 2010·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·Reyhan YeşilağaçF Z Biber Müftüler
Apr 27, 2010·Bioconjugate Chemistry·Inês F AntunesErik F J de Vries

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