Synthesis, biological evaluation and molecular docking study of 1-amino-2-aroylnaphthalenes against prostate cancer.
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.
['Rai|Reeta|R|', 'Dutta|Roshan Kumar|RK|', 'Singh|Surjeet|S|', 'Yadav|Dharmendra Kumar|DK|', 'Kumari|Seema|S|', 'Singh|Harpreet|H|', 'Gupta|Rinkoo Devi|RD|', 'Pratap|Ramendra|R|']
D000970:Antineoplastic Agents D017209:Apoptosis D016923:Cell Death D045744:Cell Line, Tumor D049109:Cell Proliferation D004305:Dose-Response Relationship, Drug D004354:Drug Screening Assays, Antitumor D006801:Humans D008297:Male D062105:Molecular Docking Simulation D015394:Molecular Structure D009281:Naphthalenes D011471:Prostatic Neoplasms D013329:Structure-Activity Relationship
Prostate cancer Naphthalene Cytotoxicity Apoptosis Oxidative damage