Evaluation of Cytotoxicity and Molecular Docking Studies of Phthalimide and Naphthalimide Derivatives as Potential Anticancer Agents

[摘要] Background and Objectives Cancer is the second leading cause of death in the world after cardiovasculardisease, so the aim of the present study was to investigate phthalimide and naphthalimide derivatives inorder to develop anticancer compounds.Subjects and Methods In this study, the cytotoxic activity of six phthalimed and naphthalamide derivativeswas evaluated using MTT method on three cancerous cell lines, including breast cancer (MCF-7),ovarian cancer (SKOV3) and lung cancer (A549) cell line. Molecular Docking studies were also performedto determine the binding energy and the compounds interaction with DNA as a possible target of thesecompounds.Results Based on MTT results, compound C1, a naphthalimide derivative, showed the highest cytotoxicactivity. IC50 values of this compound against MCF-7, SKOV3 and A549 cancer cell lines were 1.7, 6.2and 9.5 μM, respectively. Also, comparison of phthalimide and naphthalimide derivatives showed thatcompounds C1, C3, C5 with carboxyl group had better effects than other compounds, C2, C6, C4, whichbearing 5-amidoisophthalic acid moiety.Conclusion In general, naphthalimide derivatives showed better cytotoxicity than phthalimide derivatives.Compound C1 has the highest cytotoxic activity on all three cancer cell lines and can be furtherstudied in the development of new anti-cancer compounds.

[学科分类] 基础医学

[关键词] anti-cancer;Naphthalimide derivatives;Phthalimide derivatives;Molecular docking;MTT test