Six-membered Aromatic Nitrogen Heterocyclic Anti-Tumor Agents: Synthesis and Applications

Cancer stands as a serious malady, posing substantial risks to human well-being and survival. This underscores the paramount necessity to explore and investigate novel antitumor medications. Nitrogen-containing compounds, especially those derived from natural sources, form a highly significant category of antitumor agents. Among these, antitumor agents with six-membered aromatic nitrogen heterocycles have consistently attracted the attention of chemists and pharmacologists. Accordingly, we present a comprehensive summary of synthetic strategies and clinical implications of these compounds in this review. This entails an in-depth analysis of synthesis pathways for pyridine, quinoline, pyrimidine, and quinazoline. Additionally, we explore the historical progression, targets, mechanisms of action, and clinical effectiveness of small molecule inhibitors possessing these structural features. The compounds of interest in this review are six-membered aromatic nitrogen heterocyclic anti-tumor agents. We summarized the synthetic strategies of pyridine, quinoline, pyrimidine, and quinazoline, as well as an exploration of the historical progression, targets, mechanism of actions, and clinical effectiveness of small molecule inhibitors possessing these structural features.+image