Nitrogen-Based Heterocycles in Anticancer Drug Discovery: A Comprehensive Review
DOI:
https://doi.org/10.63001/tbs.2026.v21.i02.S.I(2).pp220-226Keywords:
Nitrogen heterocycles, anticancer agents,, EGFR inhibitors, synthetic strategies,, molecular pharmacology, structure–activity, relationship.Abstract
Nitrogen-based heterocyclic compounds represent a cornerstone of modern medicinal chemistry due to
their structural diversity, synthetic accessibility, and broad pharmacological activities. Recent advances
in rational drug design have emphasized heterocyclic scaffolds such as pyrazoles, indazoles,
benzothiazoles, triazoles, and benzimidazoles for anticancer drug discovery. This review summarizes
contemporary developments in the design, synthesis, characterization, and biological evaluation of
nitrogen-containing heterocycles with a focus on target-specific anticancer mechanisms such as
epidermal growth factor receptor (EGFR) inhibition. Emerging synthetic approaches including
asymmetric aza-Michael reactions, multicomponent strategies, and diversity-oriented synthesis are
discussed alongside molecular pharmacology and structure–activity relationships. The review
highlights current challenges and proposes future directions for developing safer and more effective
heterocyclic anticancer agents.
