A study of N-Heterocycles in Anticancer Drug Discovery from 2020-2024

Abstract

Nitrogen-containing heterocycles remain among the most productive scaffolds in anticancer drug discovery because they tune physicochemical properties, allow key hydrogen-bonding interactions, and support diverse modes of target engagement. Between 2020 and 2024 there was sustained medicinal-chemistry activity across classical scaffolds (indoles, quinolines/quinazolines, benzimidazoles, pyridines/pyrimidines, triazoles) and substantial clinical progress for KRAS-G12C inhibitors — small molecules built on heterocyclic cores — alongside many kinase and tubulin-targeting heterocycles advancing in trials. This study distils the 2020–2024 literature to illustrate scaffold-target pairings, SAR trends, recent approvals, and future directions.