Development of 18F-Labeled Picolinamide Probes for PET Imaging of Malignant Melanoma

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• 作者：Hongguang Liu ; Shuanglong Liu ; Zheng Miao ; Zixin Deng ; Baozhong Shen ; Xuechuan Hong ; Zhen Cheng
• 刊名：Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：February 14, 2013
• 年：2013
• 卷：56
• 期：3
• 页码：895-901
• 全文大小：293K
• 年卷期：v.56,no.3(February 14, 2013)
• ISSN：1520-4804

文摘

Melanoma is an aggressive skin cancer with worldwide increasing incidence. Development of positron emission tomography (PET) probes for early detection of melanoma is critical for improving the survival rate of melanoma patients. In this research, ¹⁸F-picolinamide-based PET probes were prepared by direct radiofluorination of the bromopicolinamide precursors using no-carrier-added ¹⁸F-fluoride. The resulting probes, ¹⁸F-1, ¹⁸F-2 and ¹⁸F-3, were then evaluated in vivo by small animal PET imaging and biodistribution studies in C57BL/6 mice bearing B16F10 murine melanoma tumors. Noninvasive small animal PET studies demonstrated excellent tumor imaging contrasts for all probes, while ¹⁸F-2 showed higher tumor to muscle ratios than ¹⁸F-1 and ¹⁸F-3. Furthermore, ¹⁸F-2 demonstrated good in vivo stability as evidenced by the low bone uptake in biodistribution studies. Collectively, these findings suggest ¹⁸F-2 as a highly promising PET probe for translation into clinical detection of melanoma.