Cytotoxicity evaluation of a new series of naphthalimide derivatives against human cancer cell lines

Abstract

Introduction: Cancer has been known as one the main causes of the death in the world. In recent researches, discovery of effective, selective and safe medications is a priority and emergency. In recent reports, the role of lipoxygenases (LOX) has been confirmed in neoplastic diseases. Some isoenzymes such as 5, 12 and 15 have more importance in the neoplasia. According to the efficacy of naphthalimides as LOX inhibitor, herein we explored the cytotoxicity of naphthalimide derivatives. Methods: A basic study was carried out in the current research. The cytotoxicity of a new series of naphthalimide-based 15-LOX-1 inhibitors was evaluated in three cancerous cell lines namely SKNMC (neuroblastoma), PC3 (prostatic cancer), HT29 (colorectal cancer) using MTT protocol and the obtained data was compared to doxorubicin. Calculation of the IC50 of tested compounds was performed by regression analysis using Prism-6 software. Results: Totally, all tested compounds exhibited inferior activity than doxorubicin towards HT-29, SKNMC and PC3 cell lines. SKNMC cell line rendered more sensitivity to tested compounds. Amongst the compounds 3a-3m, compound 3e (3-methoxy) and 3i (4-F) with IC50 = 5.92±1.78 µM and 10.04±1.7 µM were the most potent derivatives towards PC3 cells. Conclusion: Although all compounds did not exert more potency in comparison with doxorubicin, some of them showed remarkable cytotoxicity. The potent derivatives could be introduced as novel lead compounds for development of new anticancer drugs.