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放射性标记的联苯磺酰胺基质金属蛋白酶抑制剂作为新型潜在PET癌症成像剂的合成

Synthesis of radiolabeled biphenylsulfonamide matrix metalloproteinase inhibitors as new potential PET cancer imaging agents.

作者信息

Fei Xiangshu, Zheng Qi Huang, Liu Xuan, Wang Ji Quan, Sun Hui Bin, Mock Bruce H, Stone K Lee, Miller Kathy D, Sledge George W, Hutchins Gary D

机构信息

Department of Radiology, Indiana University School of Medicine, IN 46202, Indianapolis, USA.

出版信息

Bioorg Med Chem Lett. 2003 Jul 7;13(13):2217-22. doi: 10.1016/s0960-894x(03)00382-2.

DOI:10.1016/s0960-894x(03)00382-2
PMID:12798337
Abstract

Novel matrix metalloproteinase (MMP) inhibitor radiotracers, (S)-3-methyl-2-(2',3',4'-methoxybiphenyl-4-sulfonylamino)-butyric acid [(11)C]methyl ester (1a-c), (S)-3-methyl-2-(2',3',4'-fluorobiphenyl-4-sulfonylamino)-butyric acid [(11)C]methyl ester (1d-f), and (S)-3-methyl-2-(4'-nitrobiphenyl-4-sulfonylamino)-butyric acid [(11)C]methyl ester (1g), a series of substituted biphenylsulfonamide derivatives, have been synthesized for evaluation as new potential positron emission tomography (PET) cancer imaging agents.

摘要

新型基质金属蛋白酶(MMP)抑制剂放射性示踪剂,(S)-3-甲基-2-(2',3',4'-甲氧基联苯-4-磺酰氨基)-丁酸[(11)C]甲酯(1a-c)、(S)-3-甲基-2-(2',3',4'-氟联苯-4-磺酰氨基)-丁酸[(11)C]甲酯(1d-f)以及(S)-3-甲基-2-(4'-硝基联苯-4-磺酰氨基)-丁酸[(11)C]甲酯(1g),一系列取代联苯磺酰胺衍生物,已被合成用于评估作为新型潜在的正电子发射断层扫描(PET)癌症成像剂。

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