Department of Chemistry, Biochemistry Division, Faculty of Science, Cairo University, Giza 12613, Egypt.
Department of Chemistry, Faculty of Science, Islamic University of Madinah, Madinah 42351, Saudi Arabia.
Molecules. 2023 May 23;28(11):4270. doi: 10.3390/molecules28114270.
Many literature reports revealed the anticancer activity of pyridine and thiazole derivatives, especially in lung cancer. Therefore, a new series of thiazolyl pyridines linked with thiophene moiety via hydrazone group was prepared by one-pot multi-component reaction of ()-1-(4-methyl-2-(2-(1-(thiophen-2-yl)ethylidene)hydrazinyl)thiazol-5-yl)ethanone with benzaldehyde derivatives and malononitrile in a good yield. Then, compound and the thiazolyl pyridines were investigated for their in vitro anticancer activity against lung cancer (A549) cell line using MTT assay compared to doxorubicin as a reference drug. The structure of all the newly synthesized compounds was established based on spectroscopic data and elemental analyses. For better insight to investigate their mechanism of action on A549 cell line, docking studies were performed, targeting epidermal growth factor receptor (EGFR) tyrosine kinase. The results obtained revealed that the tested compounds displayed excellent anticancer activities against lung cancer cell line except and compared to reference drug. Based on the data obtained, it can be inferred that the novel compounds, as well as their key intermediate, compound , demonstrated potent anticancer activity against lung carcinoma by inhibiting EGFR.
许多文献报道表明吡啶和噻唑衍生物具有抗癌活性，特别是在肺癌方面。因此，通过一锅多组分反应，由（）-1-（4-甲基-2-（2-（1-（噻吩-2-基）亚乙基）腙基）噻唑-5-基）乙酮与苯甲醛衍生物和丙二腈制备了一系列噻唑基吡啶与噻吩部分通过腙基团连接的新化合物，产率良好。然后，通过 MTT 测定法，将化合物和噻唑基吡啶与阿霉素作为参考药物进行体外抗癌活性对肺癌（A549）细胞系的研究。所有新合成化合物的结构均基于光谱数据和元素分析确定。为了更好地研究它们对 A549 细胞系的作用机制，进行了对接研究，针对表皮生长因子受体（EGFR）酪氨酸激酶。结果表明，除了与参比药物相比，测试的化合物对肺癌细胞系表现出优异的抗癌活性。根据获得的数据，可以推断出新型化合物及其关键中间体化合物作为 EGFR 的抑制剂，对肺癌具有很强的抗癌活性。
