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

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.