Iodinated Choline Transport-Targeted Tracers.

ID: ALA5260851

Journal: J Med Chem

Title: Iodinated Choline Transport-Targeted Tracers.

Authors: Švec P, Nový Z, Kučka J, Petřík M, Sedláček O, Kuchař M, Lišková B, Medvedíková M, Kolouchová K, Groborz O, Loukotová L, Konefał RŁ, Hajdúch M, Hrubý M.

Abstract: We present a novel series of radioiodinated tracers and potential theranostics for diseases accompanied by pathological function of proteins involved in choline transport. Unlike choline analogues labeled with ¹¹C or ¹⁸F that are currently used in the clinic, the iodinated compounds described herein are applicable in positron emission tomography, single-photon emission computed tomography, and potentially in therapy, depending on the iodine isotope selection. Moreover, favorable half-lives of iodine isotopes result in much less challenging synthesis by isotope exchange reaction. Six of the described compounds were nanomolar ligands, and the best compound possessed an affinity 100-fold greater than that of choline. Biodistribution data of ¹²⁵I-labeled ligands in human prostate carcinoma bearing (PC-3) mice revealed two compounds with a biodistribution profile superior to that of [¹⁸F]fluorocholine.

CiteXplore: 33271015

DOI: 10.1021/acs.jmedchem.0c01710

Patent ID: ┄