Advanced Radiological Sciences, Department of Radiology, The University of Texas Southwestern Medical Center at Dallas , 5323 Harry Hines Boulevard, Dallas, Texas 75390-9058, United States.
J Med Chem. 2012 Aug 9;55(15):6814-21. doi: 10.1021/jm300520q. Epub 2012 Jul 27.
pH plays an important role in tumor proliferation, angiogenesis, metabolic control, and the efficacy of cytotoxic therapy, and accurate noninvasive assessment of tumor pH promises to provide insight into developmental processes and prognostic information. In this paper, we report the design, synthesis, and characterization of two novel pH indicators 6-trifluoromethylpyridoxine 8 and α(4),α(5)-di-O-[3'-O-(β-d-glucopyranosyl)propyl]-6-trifluoromethylpyridoxine 17 and demonstrate 8 as an extracellular (19)F NMR pH probe to assess pH(e) of various tumors in vivo.
pH 在肿瘤增殖、血管生成、代谢控制和细胞毒性治疗的疗效中起着重要作用，准确的无创评估肿瘤 pH 值有望提供对发育过程和预后信息的深入了解。在本文中，我们报告了两种新型 pH 指示剂 6-三氟甲基吡哆醇 8 和 α(4),α(5)-二-O-[3'-O-(β-d-吡喃葡萄糖基)丙基]-6-三氟甲基吡哆醇 17 的设计、合成和表征，并证明 8 作为一种细胞外 (19)F NMR pH 探针，可用于评估体内各种肿瘤的 pH(e)。
