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

被引:4
|
作者
Hovsepyan, T. R. [1 ]
Dilanyan, S. V. [1 ]
Minasyan, N. S. [2 ]
Arsenyan, F. G. [1 ]
Nersesyan, L. E. [1 ]
Agaronyan, A. S. [1 ]
Danielyan, I. S. [1 ]
机构
[1] Natl Acad Sci Republ Armenia, Mnjoyan Inst Fine Organ Chem, Sci & Technol Ctr Organ & Pharmaceut Chem, Pr Azatutyan 26, Yerevan 0014, Armenia
[2] Natl Acad Sci Republ Armenia, Sci & Technol Ctr Organ & Pharmaceut Chem, Mol Struct Res Ctr, Yerevan, Armenia
关键词
1,2,4-triazoles; thione-thiol tautomerism; thioether group; sarcoma-180; DNA methylation;
D O I
10.1134/S1070363218070071
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
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 N-2 atom. The synthesized compounds were studied for anti-tumor activity and the effect on the methylation level of tumor DNA.
引用
收藏
页码:1390 / 1396
页数:7
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