Starting with our previously reported work, a novel series of 3,4-dihydro-2H-[1,4]oxazino[2,3-f]quinazolin-derivatives were designed, synthesized and evaluated as potent EGFR tyrosine kinase inhibitors. All of the compounds showed significant inhibitory activities against EGFR^wt kinase (IC₅₀ ≤ 937.7 nM). Among them, compound 7j demonstrated the most potent inhibitory activity toward EGFR^wt tyrosine kinase with IC₅₀ value of 25.69 nM and showed good antiproliferative activities against NCI-H1563 and H1975 cells. The median cytotoxic concentration (CC₅₀) showed that most of the tested compounds displayed almost no cytotoxicity in vitro against 16HBE cells. In view of the reported compounds activity, the structure deserves further optimization as cancer treatment agents.

从我们之前报道的工作开始，设计、合成并评估了一系列新的 3,4-二氢-2 H -[1,4]恶嗪并[2,3- f ]喹唑啉衍生物作为有效的 EGFR 酪氨酸激酶抑制剂。^{所有化合物均显示出对 EGFR wt}激酶的显着抑制活性(IC ₅₀  ≤ 937.7 nM)。其中，化合物7j对EGFR ^wt酪氨酸激酶表现出最强的抑制活性，IC ₅₀值为25.69 nM，对NCI-H1563和H1975细胞表现出良好的抗增殖活性。中值细胞毒性浓度 (CC ₅₀) 表明，大多数测试化合物在体外对 16HBE 细胞几乎没有细胞毒性。鉴于报道的化合物活性，该结构作为癌症治疗剂值得进一步优化。