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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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Lang C,Maschauer S,Hübner H,Gmeiner P,Prante O

doi

10.1021/jm401491e

subject

Has Abstract

pub_date

2013-11-27 00:00:00

pages

9361-5

issue

22

eissn

0022-2623

issn

1520-4804

journal_volume

56

pub_type

杂志文章

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