Synthesis and In vitro Testing of Novel Quinoline Derivatives and for Cancer Cells

Kuldeep Singh Patel, Richa Dubey, Archana Singh
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Abstract

Quinoline and its derivatives represent an important class of nitrogen containing heterocycles because they are useful intermediates in organic synthesis and biological activities such as antiasthmatic, anti-inflammatory, anti- cancer, and antimalarial activity. A quinoline containing eight compounds was successfully synthesized and characterized by FT-IR, 1H NMR, 13C NMR and mass spectral analysis. Therefore, the synthesis of new quinoline derivatives with strong pharmacological activity is important in medicine. There is significant research focused on the development of new quinoline-based structures and new methods of synthesis. In this research study, new quinoline derivatives were synthesized and the synthesized compounds were characterized by several spectroscopic techniques, the biological activity of these compounds was evaluated using lung cancer cell lines and molecular modeling in an enzymatic system. The synthesized eight new compounds were tested for their potential activity in lung cancer cell lines. Eight synthesized compounds (K1- K8) were evaluated for their cytotoxic activities. The anticancer test showed that the quinoline compounds K2, K3 and K4 show good anticancer activity. Among them, K2 and K4 were shown to be dose-dependent, with K4 having the highest toxicity at 250 µM and K8 having the highest toxicity at 125, 250, and 500 µM, while K1, K2, K5, K6, and K7 were not cytotoxic.
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新型喹啉衍生物的合成及对癌细胞的体外检测
喹啉及其衍生物是一类重要的含氮杂环化合物,在有机合成和生物活性中具有重要的中间体作用,如平喘、抗炎、抗癌和抗疟疾等。成功合成了一种含有8个化合物的喹啉化合物,并通过FT-IR、1H NMR、13C NMR和质谱分析对其进行了表征。因此,合成具有较强药理活性的新型喹啉衍生物在医学上具有重要意义。新的喹啉基结构和新的合成方法的开发是重要的研究重点。在本研究中,合成了新的喹啉衍生物,并用多种光谱技术对合成的化合物进行了表征,并利用肺癌细胞株和酶系统分子模拟对这些化合物的生物活性进行了评价。对合成的8种新化合物在肺癌细胞系中的潜在活性进行了测试。对合成的8个化合物(K1- K8)进行了细胞毒活性评价。抗癌实验表明,喹啉类化合物K2、K3和K4具有良好的抗癌活性。其中,K2和K4呈剂量依赖性,K4在250µM时毒性最大,K8在125、250和500µM时毒性最大,而K1、K2、K5、K6和K7无细胞毒性。
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