A series of functionalized naphthalene was synthesized and screened against human prostate cancer cell line (PC-3). The in vitro antiproliferative activity of the synthesized compounds was evaluated by monitoring their cytotoxic effects against PC-3 cells by using MTT assay. We observed that compound 5f resulted in more than 50% cell death at 14 µM. Treatment of PC-3 cells with 5f provides apoptosis by flow cytometry. Western blotting showed decreased expression of pro-caspase 8 and 9. Our study shows that cancer cell treated with 5f has higher concentration of reactive oxygen species as compare to untreated sample, which facilitate cancerous cell to enter apoptosis. Exact mechanism by which ROS is generated after 5f treatment is still under study. Molecular docking study further strengthens the results obtained from in vitro experiments. Compound 5f can be considered as a promising leads for anticancer agent against prostate cancer cells due to its potent cytotoxic activity and apoptotic effect.

合成了一系列功能化的萘，并针对人前列腺癌细胞系（PC-3）进行了筛选。在体外合成的化合物的抗增殖活性通过使用MTT测定监测针对PC-3细胞中的细胞毒性作用进行评价。我们观察到，化合物5f在14 µM时导致50％以上的细胞死亡。用5f处理PC-3细胞可通过流式细胞仪检测细胞凋亡。Western印迹显示前胱天蛋白酶8和9的表达降低。我们的研究表明，与未处理的样品相比，用5f处理的癌细胞具有较高的活性氧浓度，这有助于癌细胞进入凋亡状态。5f后产生ROS的确切机理治疗仍在研究中。分子对接研究进一步加强了体外实验的结果。化合物5f由于其强大的细胞毒活性和凋亡作用，可以被认为是针对前列腺癌细胞的抗癌剂的有希望的先导。