College of Chemistry, Beijing Normal University, No. 19 Xinjiekouwai Street, Haidian District, Beijing 100875, China.
College of Chemistry and Chemical Engineering, Anyang Normal University, No. 436 Xian'ge Road, Anyang 455000, Henan Province, China.
Mol Pharm. 2021 Apr 5;18(4):1634-1642. doi: 10.1021/acs.molpharmaceut.0c01088. Epub 2021 Mar 19.
There are two important topics in the field of cancer research: one is targeted molecular therapy and the other is tumor molecular imaging. Focal adhesion kinase (FAK) is considered as an attractive target for oncologic diagnosis and therapy. A series of 2,4-diaminopyrimidine derivatives were labeled with F to study their biological properties and their potential as positron emission tomography tumor imaging agents. They inhibited the activity of FAK with IC values in the wide range of 0.6-2164 nM, among which the IC of was 3.2 nM. For the biodistribution in S180-bearing mice, the corresponding was relatively good, with the highest uptake of 3.35 ± 0.32 % ID/g at 30 min postinjection, with a tumor/muscle ratio of 2.08 and a tumor/bone ratio of 2.48. Accordingly, was considered as a potential PET imaging agent for tumor diagnosis.
一个是靶向分子治疗，另一个是肿瘤分子成像。黏着斑激酶（FAK）被认为是肿瘤诊断和治疗的一个有吸引力的靶点。一系列 2,4-二氨基嘧啶衍生物被标记为 F，以研究它们的生物学特性及其作为正电子发射断层扫描肿瘤成像剂的潜力。它们抑制 FAK 的活性，IC 值范围很宽，为 0.6-2164 nM，其中 的 IC 值为 3.2 nM。在 S180 荷瘤小鼠中的生物分布中，相应的 相对较好，在注射后 30 分钟时，最高摄取率为 3.35 ± 0.32 % ID/g，肿瘤/肌肉比为 2.08，肿瘤/骨比为 2.48。因此， 被认为是一种潜在的用于肿瘤诊断的 PET 成像剂。
