Molecules (May 2023)

Antitumor Activity of s-Triazine Derivatives: A Systematic Review

  • Qiuzi Dai,
  • Qinsheng Sun,
  • Xiaorong Ouyang,
  • Jinyang Liu,
  • Liye Jin,
  • Ahao Liu,
  • Binsheng He,
  • Tingting Fan,
  • Yuyang Jiang

DOI
https://doi.org/10.3390/molecules28114278
Journal volume & issue
Vol. 28, no. 11
p. 4278

Abstract

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1,3,5-triazine derivatives, also called s-triazines, are a series of containing-nitrogen heterocyclic compounds that play an important role in anticancer drug design and development. To date, three s-triazine derivatives, including altretamine, gedatolisib, and enasidenib, have already been approved for refractory ovarian cancer, metastatic breast cancer, and leukemia therapy, respectively, demonstrating that the s-triazine core is a useful scaffold for the discovery of novel anticancer drugs. In this review, we mainly focus on s-triazines targeting topoisomerases, tyrosine kinases, phosphoinositide 3-kinases, NADP+-dependent isocitrate dehydrogenases, and cyclin-dependent kinases in diverse signaling pathways, which have been extensively studied. The medicinal chemistry of s-triazine derivatives as anticancer agents was summarized, including discovery, structure optimization, and biological applications. This review will provide a reference to inspire new and original discoveries.

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