Synthesis of New Anthraquinone Derivatives and Anticancer Effects on Breast Cancer Cell Lines

Abstract

Antraquinoneand their analogues are among the important compounds investigated to developnovel bioactive and biocompatible molecules with potential for medicalapplications. The most important quinone class as anthraquinones occur widelyin plants such as aloe vera and tipton's weed. Anthraquinone derivatives havearoused special interest since they have demonstrated potential therapeuticuses as antibacterial, antiviral, antifungal agents and other biologicalactivities. Mitoxantrone, an anthraquinone analogue, is known as a syntheticanticancer analog of anthracycline antibiotics. Mitoxantrone as anticancer drugis a powerful inhibitor of the enzyme that is in charge with the repair ofdamaged DNA. In this study, new anthraquinone derivatives([1-(4-Chlorothiophenyl)-9,10-dioxoanthraquinone],[1-(4-Aminothiophenyl)-9,10dioxoanthraquinone]) were characterized by spectroscopic methods (1H-NMR,13C-NMR, FT-IR, UV-Vis analyzes). Breast cancer cell lines (MDA- MB-231 andMCF-7) and human umbilical vein endothelial cells (HUVECs) were proliferated in standard culture conditions. Cells were incubatedwith these derivatives for 24 and 48 h with in different concentrations. Cellproliferation assays, MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-DiphenyltetrazoliumBromide) and CCK-8 (Cell Counting Kit-8), were performed to reveal anticancereffect of new anthraquinone derivatives. As a result, Cell viability of MDA-MB-231 and MCF-7 cells were decreased significantly (p<0.05) by newanthraquinone derivatives treatment whereas cytotoxic effect was not observedin HUVECs. In this study new synthesized anthraquinone derivatives were testedand comparable results were observed both in vitro cytotoxicity assay andstatistical analysis. This anthraquinone derivatives are promising for itsfurther development as an anticancer drug.