Synthesis and Evaluation of a 18F-Labeled Diarylpyrazole Glycoconjugate for the Imaging of NTS1-Positive Tumors

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• 作者：Christopher Lang ; Simone Maschauer ; Harald H眉bner ; Peter Gmeiner ; Olaf Prante
• 刊名：Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：November 27, 2013
• 年：2013
• 卷：56
• 期：22
• 页码：9361-9365
• 全文大小：262K
• 年卷期：v.56,no.22(November 27, 2013)
• ISSN：1520-4804

文摘

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 [¹⁸F]8 with excellent stability and highly beneficial biodistribution in vivo as demonstrated by PET imaging in HT29 tumor-bearing nude mice. Thus, the tracer [¹⁸F]8 represents a highly promising candidate for PET imaging of NTS1-positive tumors.