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

来源：

RUSSIAN JOURNAL OF GENERAL CHEMISTRY | 2018年 / 88卷 / 07期

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

页码：1390 / 1396

页数：7

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