New DNA Methylation Inhibitors Based on 1,2,4-Triazole Thioether Derivatives

Abstract

New 4-substituted 4H-1,2,4-triazole-3-thiol derivatives were synthesized by introducing benzylsulfanylethyl groups in the 5-position of the heterocycle. Alkylation of the thiol group provides additional pharmacophore thioether, carboxamide, carboxyl, and hydroxyethyl fragments. Regardless of the nature of the substituents in the position 5 aminomethylation and cyanoethylation proceed at the N₂ atom. The synthesized compounds were studied for anti-tumor activity and the effect on the methylation level of tumor DNA.