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首页> 外文期刊>RSC Advances >Synthesis and evaluation of novel F-18-labeled pyrimidine derivatives: potential FAK inhibitors and?PET imaging agents for cancer detection
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Synthesis and evaluation of novel F-18-labeled pyrimidine derivatives: potential FAK inhibitors and?PET imaging agents for cancer detection

机译：新型F-18标记的嘧啶衍生物的合成和评估：潜在的FAK抑制剂和用于癌症检测的PET成像剂

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Based on computer-assisted drug design, a series of novel pyrimidine derivatives was successfully synthesized and characterized by 1H NMR, 13C HNMR, and MS spectra. All the new compounds were evaluated for their activity against focal adhesion kinase and showed low IC50 values in comparison with control drugs. In particular, for compound 8i, its IC50 value was 0.060 μM, suggesting its advantage as a focal adhesion kinase inhibitor. To evaluate the potentiality of these compounds as PET imaging agents in cancer detection, compounds 8a, 8c, 8h, and 8i were successively labeled with 18F. The four 18F-labeled pyrimidine derivatives showed appropriate log?P values and high stability in physiological saline and mouse plasma. Noticeably, compound [18F]-8a with a 4-methoxyl group at the benzene ring exhibited good in vivo biodistribution data in mice bearing the S180 tumor, which promoted a further microPET imaging study of compound [18F]-8a. The microPET image of [18F-8a] administered into the S180 tumor-bearing mice acquired at 60 min post-injection illustrated that the uptake in S180 tumor was obvious. These results suggested that compound [18F]-8a might be a new probe for PET tumor imaging.
机译：在计算机辅助药物设计的基础上，成功合成了一系列新型嘧啶衍生物，并通过 1 H NMR， 13 < C 1 H NMR和MS光谱。评价了所有新化合物对粘着斑激酶的活性，与对照药物相比，它们的IC 50 值低。特别地，对于化合物8i，其IC 50 值为0.060μM，表明其作为粘着斑激酶抑制剂具有优势。为了评估这些化合物作为PET显像剂在癌症检测中的潜力，先后用 18 F标记了化合物8a，8c，8h和8i。四种 18 F标记的嘧啶衍生物在生理盐水和小鼠血浆中均显示适当的log？ P 值，并具有较高的稳定性。值得注意的是，在苯环上具有4-甲氧基的化合物[ 18 F] -8a在具有苯环的小鼠体内表现出良好的体内生物分布数据。 S180肿瘤，进一步促进了化合物[ 18 F] -8a的microPET成像研究。在注射后60分钟将S <180> s F-8a [ 18 F-8a]的microPET图像显示为S180肿瘤摄取明显。这些结果表明化合物[ 18 F] -8a可能是用于PET肿瘤成像的新探针。

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