Design and Synthesis of Novel 1,2,3-Triazole Derivatives as Non-Steroidal Aromatase Inhibitors for Estrogen-Responsive Breast Cancer

Aromatase inhibitors (AIs) exhibit promising characteristics as therapeutic agents for estrogen-dependent breast cancer by inhibiting aromatase, the essential enzyme responsible for estrogen biosynthesis. The currently approved AIs for breast cancer therapy by the Food and Drug Administration are associated with significant adverse effects. Therefore, the development of novel AIs with enhanced specificity and potency is crucial. This study describes the synthesis and characterization of new nonsteroidal aromatase inhibitors incorporating triazole moieties, intended for the management of hormone-dependent breast cancer in postmenopausal women. A series of 1,2,3-triazole-based compounds was successfully prepared, and their structures were confirmed using spectral data (FT-IR, ¹³C NMR, ¹H NMR, mass spectrometry) and elemental analysis. The physical properties of these novel derivatives were also documented. The compounds were evaluated for anticancer activity in breast cancer cell lines (MCF7 and T-47D) as well as in a normal breast cell line (MCF 10A), assessing their impact on cell proliferation, migration, and invasion. The findings indicate that these compounds demonstrate promising and selective anticancer effects.