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Detection of apoptosis by PET/CT with the diethyl ester of [18F]ML-10 and fluorescence imaging with a dansyl analogue

Authors :
Gavin Brown
Muhammad Babur
Alison Smigova
Christopher Cawthorne
Kaye J. Williams
Paul Birkket
Manikandan Kadirvel
Emily J. Rowling
Michael Fairclough
Adam McMahon
Sally Freeman
Source :
Bioorganic & Medicinal Chemistry. 22:341-349
Publication Year :
2014
Publisher :
Elsevier BV, 2014.

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.

Details

ISSN :
09680896
Volume :
22
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry
Accession number :
edsair.doi...........cb2d029480028deca027fa40e2445bd3
Full Text :
https://doi.org/10.1016/j.bmc.2013.11.019