In view of the important role of quinazoline skeletons in anti-cancer drugs like Gefitinib and the vital importance of organoselenium compounds in biomedicine field, in this protocol, twenty quinazoline selenium derivatives were designed and synthesized with the aim to develop new anti-cancer drugs by utilizing the synergistic effects of quinazoline skeleton and selenium. In addition, the synthetic method of thioether substituted quinazolines was improved. The biological activities of title compounds were determined against A549 cancer cells in vitro by using MTT assay at 1 μM and 10 μM concentrations. The results showed that most of the title compounds had good anticancer activities. Of note, 6-chloro-4-benzylselenoquinazoline (G5) exhibited better inhibitory activity (67.8% inhibition ratio) than the positive control drug Gefitinib (62.9% inhibition ratio) at the concentration of 10 μM. These findings will provide some clues for further research of anticancer drugs.

中文翻译：

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硒/硫醚喹唑啉化合物的合成及生物活性

鉴于喹唑啉骨架在吉非替尼等抗癌药物中的重要作用以及有机硒化合物在生物医学领域的重要性，本方案设计合成了20种喹唑啉硒衍生物，旨在开发抗癌新药。利用喹唑啉骨架和硒的协同作用。此外，改进了硫醚取代喹唑啉的合成方法。通过使用 MTT 法在 1 μM 和 10 μM 浓度下测定标题化合物对 A549 癌细胞的体外生物活性。结果表明，大部分标题化合物具有良好的抗癌活性。值得注意的是，6-chloro-4-benzylseenoquinazoline ( G 5) 在 10 μM 浓度下表现出比阳性对照药物吉非替尼 (62.9% 抑制率) 更好的抑制活性 (67.8% 抑制率)。这些发现将为进一步研究抗癌药物提供一些线索。