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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 :
Manikandan, Kadirvel
Michael, Fairclough
Christopher, Cawthorne
Emily J, Rowling
Muhammad, Babur
Adam, McMahon
Paul, Birkket
Alison, Smigova
Sally, Freeman
Kaye J, Williams
Gavin, Brown
Source :
Bioorganicmedicinal chemistry. 22(1)
Publication Year :
2013

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 :
14643391
Volume :
22
Issue :
1
Database :
OpenAIRE
Journal :
Bioorganicmedicinal chemistry
Accession number :
edsair.pmid..........1523dad921b839e0a93b6870621e16ed