Synthesis, Ant Proliferative Activity and Docking Study of New Quercetin Derivatives against MDA-MB231 Breast Cancer Cell Lines

Abstract

MDA-MB231 is a very aggressive and invasive triple negative breast cancer, which present with limited treatment options. Unlike other breast cancer types, it is characterized by absence of hormonal receptors of estrogen, progesterone as well as human epidermal growth factor receptor 2, rendering it unsuitable for hormonal therapy and a perfect candidate for chemotherapy. Quercetin is a common natural flavonoid present in many food items, which have a wide range of biological activities, likes anticancer, antiviral, antibacterial and antioxidant. This study involves the synthesis of new Quercetin derivatives and the investigation their effects against MDA-MB231 cell lines. The structures of the derivatives were established using UV, IR, ¹HNMR, CHNS, EIMS and ESIMS techniques. Their antiproliferative activities were investigated in vitro using Microculture Tetrazolium (MTT) assay. The percentage cell viability following exposure to Quercetin and its derivatives (Compounds 1-5) were measured. Both compounds 1 and 4 show a significant decrease in percentage cell viability from 100% to 43.7% and 38.1% respectively. IC₅₀ value was calculated for compound 1 and 4 and found to be 2.042 and 1.838 µM respectively, indicating that they have a potential anticancer activity against the triple negative breast cancer type. The antiproliferative activity was supported and evidenced by molecular docking study.