18F-Fluorination of Unactivated C-H Bonds in Branched Aliphatic Amino Acids: Direct Synthesis of Oncological Positron Emission Tomography Imaging Agents.
Matthew B NodwellHua YangMilena ČolovićZheliang YuanHelen MerkensRainer E MartinFrançois BénardPaul SchafferRobert A BrittonPublished in: Journal of the American Chemical Society (2017)
A mild and selective photocatalytic C-H 18F-fluorination reaction has been developed that provides direct access to 18F-fluorinated amino acids. The biodistribution and uptake of three 18F-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.
Keyphrases
- positron emission tomography
- pet imaging
- computed tomography
- amino acid
- high resolution
- pet ct
- prostate cancer
- papillary thyroid
- small molecule
- molecular docking
- rectal cancer
- high throughput
- radical prostatectomy
- benign prostatic hyperplasia
- high fat diet induced
- gold nanoparticles
- quantum dots
- minimally invasive
- skeletal muscle
- fluorescence imaging