title: 18F-Fluorination of Unactivated C-H Bonds in Branched Aliphatic Amino Acids: Direct Synthesis of Oncological Positron Emission Tomography Imaging Agents.
abstract: A mild and selective photocatalytic C-H18F-fluorination reaction has been developed that provides direct access to18F-fluorinated amino acids. The biodistribution and uptake of three18F-labeled leucine analogues via LAT1 mediated transport in several cancer cell lines is reported. Positron emission tomography imaging of mice bearing PC3 (prostate) or U87 (glioma) xenografts using 5-[18F]-fluorohomoleucine showed high tumor uptake and excellent tumor visualization, highlighting the utility of this strategy for rapid tracer discovery for oncology.
authors.affiliation: Department of Chemistry, Simon Fraser University , Burnaby, British Columbia V5A 1S2, Canada.
authors.forename: Matthew B
authors.initials: MB
authors.lastname: Nodwell
authors.affiliation: Life Sciences Division, TRIUMF , Vancouver, British Columbia V6T 2A3, Canada.
authors.forename: Hua
authors.initials: H
authors.lastname: Yang
authors.affiliation: Department of Molecular Oncology, BC Cancer Agency , Vancouver, British Columbia V5Z 1L3 Canada.
authors.forename: Milena
authors.initials: M
authors.lastname: Čolović
authors.affiliation: Department of Chemistry, Simon Fraser University , Burnaby, British Columbia V5A 1S2, Canada.|Life Sciences Division, TRIUMF , Vancouver, British Columbia V6T 2A3, Canada.
authors.forename: Zheliang
authors.initials: Z
authors.lastname: Yuan
authors.affiliation: Department of Molecular Oncology, BC Cancer Agency , Vancouver, British Columbia V5Z 1L3 Canada.
authors.forename: Helen
authors.initials: H
authors.lastname: Merkens
authors.affiliation: Medicinal Chemistry, Roche Pharma Research and Early Development (pRED), Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd , Grenzacherstrasse 124, CH-4070 Basel, Switzerland.
authors.forename: Rainer E
authors.identifier: 0000-0001-7895-497X
authors.initials: RE
authors.lastname: Martin
authors.affiliation: Department of Molecular Oncology, BC Cancer Agency , Vancouver, British Columbia V5Z 1L3 Canada.
authors.forename: François
authors.initials: F
authors.lastname: Bénard
authors.affiliation: Department of Chemistry, Simon Fraser University , Burnaby, British Columbia V5A 1S2, Canada.|Life Sciences Division, TRIUMF , Vancouver, British Columbia V6T 2A3, Canada.
authors.forename: Paul
authors.initials: P
authors.lastname: Schaffer
authors.affiliation: Department of Chemistry, Simon Fraser University , Burnaby, British Columbia V5A 1S2, Canada.
authors.forename: Robert
authors.identifier: 0000-0002-9335-0047
authors.initials: R
authors.lastname: Britton
mesh_terms: D000596:Amino Acids / Q000737:chemistry*; D000818:Animals; D005462:Fluorine Radioisotopes; D005910:Glioma / Q000000981:diagnostic imaging*; D054879:Halogenation; D006801:Humans; D008297:Male; D051379:Mice; D008968:Molecular Conformation; D009374:Neoplasms, Experimental / Q000000981:diagnostic imaging; D049268:Positron-Emission Tomography; D011471:Prostatic Neoplasms / Q000000981:diagnostic imaging*; D011849:Radioactive Tracers; D019275:Radiopharmaceuticals / Q000737:chemistry*
chemical_list: D000596:Amino Acids; D005462:Fluorine Radioisotopes; D011849:Radioactive Tracers; D019275:Radiopharmaceuticals