Synthesis, docking study, and DNA photocleavage activity of some pyrimidinyl hydrazones and 3-(quinolin-3-yl)-5,7-dimethyl-1,2,4-triazolo[4,3-a]pyrimidine derivatives

被引：18

作者：

Sharma, Ajay ^{[1
]}

Kumar, Vinod ^{[1
]}

Khare, Rajshree ^{[1
]}

Gupta, Girish Kumar ^{[2
]}

Beniwal, Vikas ^{[3
]}

机构：

[1] Maharishi Markandeshwar Univ, Dept Chem, Ambala 133207, Haryana, India

[2] Maharishi Markandeshwar Univ, Dept Pharmaceut Chem, Maharishi Markandeshwar Coll Pharm, Ambala 133207, Haryana, India

[3] Maharishi Markandeshwar Univ, Dept Biotechnol, Ambala 133207, Haryana, India

来源：

MEDICINAL CHEMISTRY RESEARCH | 2015年 / 24卷 / 05期

基金：

英国科研创新办公室;

关键词：

Quinoline; Triazolopyrimidine; Hydrazone; (Diacetoxyiodo)benzene; DNA photocleavage activity; Docking study; POTENTIAL ANTITUMOR AGENTS; ANTIBACTERIAL ACTIVITY; INTERCALATING COMPOUNDS; CYTOTOXICITY; INHIBITORS; CLEAVAGE; DESIGN; DRUG;

D O I：

10.1007/s00044-014-1265-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In the present study, synthesis of a series of some novel 3-(Quinolin-3-yl)-5,7-dimethyl-1,2,4-triazolo[4,3-a]pyrimidine derivatives (4a-e) has been achieved by oxidative cyclization of new pyrimidinyl hydrazone intermediates (3a-e) using hypervalent iodine reagent(III) under mild conditions. The structures of all synthesized compounds were established on the basis of IR, NMR (H-1 and C-13), mass spectral data, and elemental analysis. All compounds were evaluated for their DNA photocleavage activity. Compounds 4a, 4b, 4d and 3a-e were found to possess good activity at 40 mu g/mu l concentration and were mainly responsible for the conversion of supercoiled form of DNA into open circular form. Further, docking study was carried out using Molegro Virtual Docker version 2010.4.2.0 using PDB (1AB4) in support of the results obtained.

引用

页码：1830 / 1841

页数：12

共 46 条

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