An overview on the recent developments of 1,2,4-triazine derivatives as anticancer compounds

  • Eur J Med Chem. 2017 Dec 15:142:328-375. doi: 10.1016/j.ejmech.2017.08.009.
Stella Cascioferro  1 Barbara Parrino  1 Virginia Spanò  1 Anna Carbone  1 Alessandra Montalbano  1 Paola Barraja  1 Patrizia Diana  1 Girolamo Cirrincione  2
Affiliations
  • 1. Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy.
  • 2. Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy. Electronic address: [email protected].
Abstract

The synthesis, the antitumor activity, the SAR and, whenever described, the possible mode of action of 1,2,4-triazine derivatives, their N-oxides, N,N'-dioxides as well as the benzo- and hetero-fused systems are reported. Herein are treated derivatives disclosed to literature from the beginning of this century up to 2016. Among the three possible triazine isomers, 1,2,4-triazines are the most studied ones and many derivatives having remarkable antitumor activity have been reported in the literature and also patented reaching advanced phases of clinical trials.

Keywords
1,2,4-benzotriazine; 1,2,4-triazine; Antiproliferative activity; Antitumor activity; Nitrogen heterocycles.