N²,6-Substituted 1,3,5-triazine-2,4-diamines (N²-substituted guanamines) attracted significant interest due to their potential in the development of bioactive molecules. With just two points of diversity, this scaffold is proved to be suitable for constructing compounds targeting various enzymes, receptors, transporters, and nucleic acids with an array of therapeutic applications, particularly in cancer, inflammation, and CNS disorders. This review discusses progress in the synthesis of N²,6-substituted 1,3,5-triazine-2,4-diamines and their biological activities ranging from the inhibition of cancer-related enzymes (e.g. DNA topoisomerase IIα, carbonic anhydrases, ubiquitin-conjugating enzyme 2B, lysophosphatidic acid acyltransferase β and various kinases) to the binding to CNS-relevant receptors (e.g. histamine H₄, serotonin 5-HT₆, adenosine A_2a, and α7 nicotinic acetylcholine receptors).

N ² ,6-取代的1,3,5-三嗪-2,4-二胺（N ² -取代的胍胺）因其在开发生物活性分子方面的潜力而引起了极大的兴趣。只有两点多样性，这种支架被证明适用于构建靶向各种酶、受体、转运蛋白和核酸的化合物，具有一系列治疗应用，特别是在癌症、炎症和中枢神经系统疾病中。这篇综述讨论了N ² ,6-取代的 1,3,5-triazine-2,4-diamines 的合成进展及其生物活性，从抑制癌症相关酶（例如. DNA 拓扑异构酶 IIα、碳酸酐酶、泛素结合酶 2B、溶血磷脂酸酰基转移酶 β 和各种激酶）与 CNS 相关受体（例如组胺 H ₄、血清素 5-HT ₆、腺苷 A _2a和 α7 烟碱乙酰胆碱）的结合受体）。