Lymphocyte-specific protein tyrosine kinase (Lck) plays vital roles in the -cell receptor- mediated development, function, and differentiation of -cells. Given its substantial involvement in T cell signaling, irregularities in the expression and functionality of Lck may lead to various diseases, including cancer. In this study, we found that compound exerted significant inhibitory potency against Lck with an IC value of 10.6 nM. In addition, demonstrated high efficacy in various colon cancer cell lines as indicated by GI values ranging from 0.24 to 1.26 μM. Notably, inhibited the phosphorylation of Lck in Colo201 cells. Overall, the anti-proliferative effects of on diverse cancer cell lines highlights its potential application for the treatment of various cancer types.

中文翻译：

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鉴定 3,4-二氢嘧啶并[4,5-d]pyrimidin-2(1H)-one 支架作为有效的 Lck 抑制剂作为抗癌药物

淋巴细胞特异性蛋白酪氨酸激酶 (Lck) 在细胞受体介导的细胞发育、功能和分化中发挥重要作用。鉴于 Lck 大量参与 T 细胞信号传导，Lck 表达和功能的异常可能导致多种疾病，包括癌症。在这项研究中，我们发现该化合物对 Lck 具有显着的抑制作用，IC 值为 10.6 nM。此外，GI 值范围为 0.24 至 1.26 μM，表明对各种结肠癌细胞系均具有高效功效。值得注意的是，抑制 Colo201 细胞中 Lck 的磷酸化。总体而言，对不同癌细胞系的抗增殖作用凸显了其在治疗各种癌症类型中的潜在应用。