Document Report Card

ID: ALA3085769

Journal: J Med Chem

Title: Synthesis and evaluation of a (18)F-labeled diarylpyrazole glycoconjugate for the imaging of NTS1-positive tumors.

Authors: Lang C, Maschauer S, Hübner H, Gmeiner P, Prante O.

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.

CiteXplore: 24160350

DOI: 10.1021/jm401491e