Synthesis and evaluation of a 18F-labeled diarylpyrazole glycoconjugate for the imaging of NTS1-positive tumors

Lang C, Maschauer S, Hübner H, Gmeiner P, Prante O (2013)

Publication Language: English

Publication Type: Journal article, Original article

Publication year: 2013

Journal

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

Publisher: American Chemical Society

Book Volume: 56

Pages Range: 9361-9365

Journal Issue: 22

DOI: 10.1021/jm401491e

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 [ 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 [F]8 represents a highly promising candidate for PET imaging of NTS1-positive tumors. © 2013 American Chemical Society.

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APA:

Lang, C., Maschauer, S., Hübner, H., Gmeiner, P., & Prante, O. (2013). Synthesis and evaluation of a 18F-labeled diarylpyrazole glycoconjugate for the imaging of NTS1-positive tumors. Journal of Medicinal Chemistry, 56(22), 9361-9365. https://doi.org/10.1021/jm401491e

MLA:

Lang, Christopher, et al. "Synthesis and evaluation of a 18F-labeled diarylpyrazole glycoconjugate for the imaging of NTS1-positive tumors." Journal of Medicinal Chemistry 56.22 (2013): 9361-9365.

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