Synthesis and Anticancer Activity of Imidazole and Triazole Derivatives of Flavonoids

The study involves the design and synthesis of novel flavonoid-based non-steroidal aromatase inhibitors using modified Baker-Venkataraman methods. Key structural features include imidazole and triazole heterocyclic rings that act as heme-coordinating groups, with substituents positioned to serve as hydrogen bond acceptors interacting with Serine-478 in the aromatase enzyme's active site. The synthesized compounds were characterized using IR, NMR, and Mass spectroscopy and tested for anticancer activity via SRB assay on MCF-7 breast cancer cells. Results indicate that a nitro-substituted triazole derivative exhibits significant inhibitory activity, surpassing letrozole in potency. The work contributes to the development of targeted, safe therapies for hormone-dependent breast cancer.