title: Synthesis and evaluation of a (18)F-labeled diarylpyrazole glycoconjugate for the imaging of NTS1-positive tumors.
abstract: Aiming to image NTS1 overexpressing tumors, the diarylpyrazole glycoconjugate 8, derived from the potent NTS1 antagonist SR142948A, was synthesized taking advantage of the palladium-catalyzed aminocarbonylation reaction. The glycoconjugate 8 displayed excellent affinity and selectivity toward NTS1. Radiosynthesis proceeded straightforwardly, obtaining [(18)F]8 with excellent stability and highly beneficial biodistribution in vivo as demonstrated by PET imaging in HT29 tumor-bearing nude mice. Thus, the tracer [(18)F]8 represents a highly promising candidate for PET imaging of NTS1-positive tumors.
authors.affiliation: Department of Chemistry and Pharmacy, Medicinal Chemistry, Emil Fischer Center, Friedrich Alexander University , Schuhstraße 19, 91052 Erlangen, Germany.
authors.forename: Christopher
authors.initials: C
authors.lastname: Lang
authors.forename: Simone
authors.initials: S
authors.lastname: Maschauer
authors.forename: Harald
authors.initials: H
authors.lastname: Hübner
authors.forename: Peter
authors.initials: P
authors.lastname: Gmeiner
authors.forename: Olaf
authors.initials: O
authors.lastname: Prante
mesh_terms: D000480:Alkynes / Q000737:chemistry; D000818:Animals; D001386:Azides / Q000737:chemistry; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism; D002384:Catalysis; D002471:Cell Transformation, Neoplastic; D060326:Chemistry Techniques, Synthetic; D057930:Click Chemistry; D005462:Fluorine Radioisotopes; D006001:Glycoconjugates / Q000737:chemistry*; D019073:HT29 Cells; D006801:Humans; D007553:Isotope Labeling; D051379:Mice; D008872:Microwaves; D010165:Palladium / Q000737:chemistry; D049268:Positron-Emission Tomography / Q000379:methods*; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry; D051381:Rats; D018028:Receptors, Neurotensin / Q000378:metabolism*
chemical_list: D000480:Alkynes; D001386:Azides; D005462:Fluorine Radioisotopes; D006001:Glycoconjugates; D011720:Pyrazoles; D018028:Receptors, Neurotensin; C114036:neurotensin type 1 receptor; D010165:Palladium