1. Detection of apoptosis by PET/CT with the diethyl ester of [18F]ML-10 and fluorescence imaging with a dansyl analogue
- Author
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Gavin Brown, Muhammad Babur, Alison Smigova, Christopher Cawthorne, Kaye J. Williams, Paul Birkket, Manikandan Kadirvel, Emily J. Rowling, Michael Fairclough, Adam McMahon, and Sally Freeman
- Subjects
integumentary system ,Chemistry ,Stereochemistry ,organic chemicals ,Organic Chemistry ,Clinical Biochemistry ,Radiosynthesis ,Pharmaceutical Science ,Halogenation ,complex mixtures ,Biochemistry ,Small molecule ,In vitro ,chemistry.chemical_compound ,Nucleophile ,In vivo ,Yield (chemistry) ,Drug Discovery ,Molecular Medicine ,Molecular Biology ,Fluoride ,Nuclear chemistry - Abstract
The diethyl ester of [(18)F]ML-10 is a small molecule apoptotic PET probe for cancer studies. Here we report a novel multi-step synthesis of the diethyl ester of ML-10 in excellent yields via fluorination using Xtal-Fluor-E. In addition, a one-pot radiosynthesis of the diethyl ester of [(18)F]ML-10 from nucleophilic [(18)F]fluoride was completed in 23% radiochemical yield (decay corrected). The radiochemical purity of the product was ≥99%. The diethyl ester of [(18)F]ML-10 was used in vivo to detect apoptosis in the testes of mice. In parallel studies, the dansyl-ML-10 diethyl ester was prepared and used to detect apoptotic cells in an in vitro cell based assay.
- Published
- 2014
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