Synthesis, biological evaluation and molecular docking study of 1-amino-2-aroylnaphthalenes against prostate cancer

[Display omitted] Cytotoxicity of 5f and cisplatin was measured by MTT assay. 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 cyt...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2018-05, Vol.28 (9), p.1574-1580
Main Authors: Rai, Reeta, Dutta, Roshan Kumar, Singh, Surjeet, Yadav, Dharmendra Kumar, Kumari, Seema, Singh, Harpreet, Gupta, Rinkoo Devi, Pratap, Ramendra
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Apoptosis
Apoptosis - drug effects
Cell Death - drug effects
Cell Line, Tumor
Cell Proliferation - drug effects
Cytotoxicity
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Male
Molecular Docking Simulation
Molecular Structure
Naphthalene
Naphthalenes - chemical synthesis
Naphthalenes - chemistry
Naphthalenes - pharmacology
Oxidative damage
Prostate cancer
Prostatic Neoplasms - drug therapy
Prostatic Neoplasms - pathology
Structure-Activity Relationship
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Summary:[Display omitted] Cytotoxicity of 5f and cisplatin was measured by MTT assay. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2018.03.057