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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. [ABSTRACT FROM AUTHOR]

This article, titled "Cover Picture: Six-Membered Aromatic Nitrogen Heterocyclic Anti-Tumor Agents: Synthesis and Applications," discusses the synthesis strategies and clinical applications of nitrogen-containing heterocyclic antitumor agents. The cover picture showcases various classes of these antitumor skeletons, including pyridine, quinoline, pyrimidine, and quinazoline. The article provides a detailed review of the small molecule inhibitors based on these scaffolds and their use in the field of anti-tumor research. The authors of the article are Jiatong Li, Ao Gu, Xiao-Mei Nong, Shuyang Zhai, Zhu-Ying Yue, Meng-Yao Li, and Yingbin Liu. [Extracted from the article]