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  2. A closer look at N2,6-substituted 1,3,5-triazine-2,4-diamines: Advances in synthesis and biological activities

A closer look at N2,6-substituted 1,3,5-triazine-2,4-diamines: Advances in synthesis and biological activities

  • Eur J Med Chem. 2022 Nov 5;241:114645. doi: 10.1016/j.ejmech.2022.114645.
Muhammad Syafiq Bin Shahari 1 Anton V Dolzhenko 2
Affiliations

Affiliations

  • 1 School of Pharmacy, Monash University Malaysia, Jalan Lagoon Selatan, Bandar Sunway, Selangor Darul Ehsan, 47500, Malaysia.
  • 2 School of Pharmacy, Monash University Malaysia, Jalan Lagoon Selatan, Bandar Sunway, Selangor Darul Ehsan, 47500, Malaysia; Curtin Medical School, Curtin Health Innovation Research Institute, Faculty of Health Sciences, Curtin University, GPO Box U1987 Perth, Western Australia, 6845, Australia. Electronic address: anton.dolzhenko@monash.edu.
Abstract

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 A2a, and α7 nicotinic acetylcholine receptors).

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