title: Detection of apoptosis by PET/CT with the diethyl ester of [¹⁸F]ML-10 and fluorescence imaging with a dansyl analogue.
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.
authors.affiliation: Wolfson Molecular Imaging Centre, University of Manchester, M20 3LJ, UK; Manchester Pharmacy School, University of Manchester, M13 9PT, UK.
authors.forename: Manikandan
authors.initials: M
authors.lastname: Kadirvel
authors.affiliation: Wolfson Molecular Imaging Centre, University of Manchester, M20 3LJ, UK.
authors.forename: Michael
authors.initials: M
authors.lastname: Fairclough
authors.affiliation: Wolfson Molecular Imaging Centre, University of Manchester, M20 3LJ, UK.
authors.forename: Christopher
authors.initials: C
authors.lastname: Cawthorne
authors.affiliation: Manchester Pharmacy School, University of Manchester, M13 9PT, UK.
authors.forename: Emily J
authors.initials: EJ
authors.lastname: Rowling
authors.affiliation: Wolfson Molecular Imaging Centre, University of Manchester, M20 3LJ, UK.
authors.forename: Muhammad
authors.initials: M
authors.lastname: Babur
authors.affiliation: Wolfson Molecular Imaging Centre, University of Manchester, M20 3LJ, UK.
authors.forename: Adam
authors.initials: A
authors.lastname: McMahon
authors.affiliation: School of Science and Environment, Manchester Metropolitan University, M15 6BH, UK.
authors.forename: Paul
authors.initials: P
authors.lastname: Birkket
authors.affiliation: Wolfson Molecular Imaging Centre, University of Manchester, M20 3LJ, UK.
authors.forename: Alison
authors.initials: A
authors.lastname: Smigova
authors.affiliation: Manchester Pharmacy School, University of Manchester, M13 9PT, UK.
authors.forename: Sally
authors.initials: S
authors.lastname: Freeman
authors.affiliation: Wolfson Molecular Imaging Centre, University of Manchester, M20 3LJ, UK; Manchester Pharmacy School, University of Manchester, M13 9PT, UK.
authors.forename: Kaye J
authors.initials: KJ
authors.lastname: Williams
authors.affiliation: Wolfson Molecular Imaging Centre, University of Manchester, M20 3LJ, UK. Electronic address: gavin.d.brown@manchester.ac.uk.
authors.forename: Gavin
authors.initials: G
authors.lastname: Brown
mesh_terms: D000818:Animals; D017209:Apoptosis; D004952:Esters; D005462:Fluorine Radioisotopes; D054879:Halogenation; D006801:Humans; D008297:Male; D051379:Mice; D049268:Positron-Emission Tomography / Q000379:methods*; D011854:Radiochemistry; D019275:Radiopharmaceuticals; D014057:Tomography, X-Ray Computed / Q000379:methods*
chemical_list: D004952:Esters; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals
keywords: Apoptosis; Fluorine-18; ML-10; Nucleophilic fluorination; PET/CT; XtalFluor-E