The aim of the present study is to synthesise an aryl ester compound from quinoline-2-carboxylic acid to evaluate its apoptotic, cell cycle blockade, and antiproliferative activity on the prostate cancer cell lines (PC3). Chromatographic and spectroscopic analysis was used to identify the synthesised carboxylic acid compound. The synthesised compound was treated with a PC3 cell line for 24 h with control. The cells were treated at various concentration ranges of 0, 3.91, 7.81, 15.63, 31.25, 62.5, 125, 250, 500, and 1000 µg/mL each. The cytotoxicity effect was studied by MTT assay, and their anticancer activity was further evaluated using cell cycle analysis, DNA fragmentation assay, acridine orange-ethidium bromide staining, and Western blot analysis. The end antiproliferative result showed that PC3 cell viability decreases in a concentration-dependent manner and the synthesised compound exhibited potent cytotoxicity against PC3 cells with an IC₅₀ value of 26 µg/mL at the concentration of 125 µg. The increase in the number of apoptotic cells was observed after treating PC3 cells with the sample in double-staining methods. S phase of the cell cycle was significantly blocked by the test sample, and a typical ladder pattern of internucleosomal fragmentation was observed. A decrease in the live cells was observed with the sample in AO/ET-BR. A significant increase in the Bax expression and a decrease in Bcl-2 expression observed enhance the activity of caspases-7 and -9. The synthesised compound had shown to possess excellent cytotoxic effect through inducing apoptosis, especially causing cell cycle arrest at the S phase.

本研究的目的是从喹啉-2-羧酸合成芳基酯化合物，以评估其对前列腺癌细胞系（PC3）的凋亡、细胞周期阻断和抗增殖活性。使用色谱和光谱分析来鉴定合成的羧酸化合物。将合成的化合物与对照一起用 PC3 细胞系处理 24 小时。细胞分别以 0、3.91、7.81、15.63、31.25、62.5、125、250、500 和 1000 µg/mL 的不同浓度范围进行处理。通过MTT法研究其细胞毒性作用，并通过细胞周期分析、DNA片段分析、吖啶橙-溴化乙锭染色和Western blot分析进一步评价其抗癌活性。最终的抗增殖结果表明，PC3细胞活力以浓度依赖性方式降低，合成的化合物对PC3细胞表现出有效的细胞毒性，在125 μg浓度下IC ₅₀值为26 μg/mL。用双染法处理PC3细胞后观察到凋亡细胞数量的增加。细胞周期的S期被测试样品显着阻断，并观察到典型的核小体间碎片阶梯模式。在 AO/ET-BR 中的样品中观察到活细胞减少。观察到 Bax 表达的显着增加和 Bcl-2 表达的减少增强了 caspase-7 和 -9 的活性。合成的化合物通过诱导细胞凋亡，特别是引起细胞周期阻滞在S期，具有优异的细胞毒作用。