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

Chem Rec. 2023 Dec;23(12):e202300293. doi: 10.1002/tcr.202300293. Epub 2023 Nov 27.

Abstract

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.

Keywords: Anti-tumor; Clinical application; Nitrogen-containing heterocycles; Small molecule inhibitor; Synthetic strategy.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / pharmacology
  • Heterocyclic Compounds* / chemistry
  • Heterocyclic Compounds* / pharmacology
  • Humans
  • Nitrogen / chemistry

Substances

  • Heterocyclic Compounds
  • Nitrogen
  • Antineoplastic Agents