Journal Article

Antitumor Activity of s-Triazine Derivatives: A Systematic Review

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

2023

Overview

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.

• Publisher: MDPI AG,MDPI
• Subject: Antineoplastic Agents - chemistry / Antineoplastic Agents - pharmacology / Antineoplastic Agents - therapeutic use / antitumor / Breast cancer / Breast Neoplasms / Cancer / Cancer therapies / Care and treatment / Cyclin-dependent kinases / Cytotoxicity / Dehydrogenases / Drug Design / Drug Screening Assays, Antitumor / drug target / Enzymes / Epidermal growth factor / Female / Health aspects / Heterocyclic compounds / Humans / Kinases / Leukemia / Ovarian cancer / Proteins / Review / s-triazines / Structure-Activity Relationship / Triazines - chemistry / Triazines - pharmacology / Triazines - therapeutic use / Tyrosine