ABSTRACT
This study aims to combat breast cancer, which is a significant health concern for women worldwide. By targeting aromatase, an enzyme crucial in estrogen synthesis, the research focuses on breast cancer cases, emphasizing the importance of hormonal therapy. The innovative approach of this study involves the synthesis of novel bis-triazolopyridopyrimidines, designed to amplify the combined pharmacological advantages of the pyridopyrimidine and 1,2,4-triazole structures known for their aromatase inhibition and anti-cancer capabilities. Through the synthesis and characterization of these compounds using 1H-NMR, 13C-NMR, and MS spectral analyses, and evaluating their anticancer efficacy with MTT assays against MCF-7 breast cancer cell lines in vitro, the research endeavors to develop potent aromatase inhibitors as viable anti-breast cancer agents. Identifying compounds with strong binding energies to aromatase through molecular docking analyses further supports their potential effectiveness in inhibiting aromatase activity, a key mechanism in breast cancer progression. The findings, particularly regarding compounds 5b, 5c, 10a, and 10b, which exhibited the strongest binding energies with aromatase, highlight promising candidates for further development and testing as potential therapeutic agents against breast cancer. This approach showcases the potential of these synthesized compounds in combating breast cancer by inhibiting aromatase activity.
