One-pot multicomponent synthesis of novel 1-thiazolyl-5-coumarin-3-yl-pyrazole derivatives and evaluation of their cytotoxic activity

被引：15

作者：

Velpula, Ravibabu ^{[1
]}

Deshineni, Rajitha ^{[2
]}

Gali, Rajitha ^{[1
]}

Bavantula, Rajitha ^{[1
]}

机构：

[1] Natl Inst Technol, Dept Chem, Warangal 506004, Telangana, India

[2] Osmania Univ, Dept Chem, Hyderabad 500007, Telangana, India

来源：

RESEARCH ON CHEMICAL INTERMEDIATES | 2016年 / 42卷 / 03期

关键词：

One-pot multicomponent reaction; 1-thiazolyl-5-coumarin-3-yl-pyrazole; Cytotoxic activity; BIOLOGICAL EVALUATION; ANTICANCER AGENTS; PHARMACOLOGICAL EVALUATION; ANTIMICROBIAL EVALUATION; THIAZOLE DERIVATIVES; PYRAZOLE DERIVATIVES; ANTIVIRAL ACTIVITY; DESIGN;

D O I：

10.1007/s11164-015-2114-2

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of novel 1-thiazolyl-5-coumarin-3-yl-pyrazole derivatives (4a-l) were synthesized via one-pot multicomponent reaction of 5-substituted salicylaldehydes (1a-c), 4-hydroxy-6-methyl-2H-pyran-2-one (2) and 2-hydrazinyl-4-arylthiazoles (3a-d) in acetonitrile using a catalytic amount of piperidine under reflux conditions. This multicomponent approach has advantages such as reduced reaction time and a high product yield percentage when compared with corresponding multistep approaches. All the synthesized compounds were evaluated for their cytotoxic activity against Hep G2 (hepatocellular liver carcinoma) and MCF-7 (breast cancer) cell lines and compared with the standard drug Doxorubicin. Among all the compounds, compounds 4d against Hep G2, 4k against MCF-7 and 4e against both Hep G2 & MCF-7 showed excellent cytotoxic activity.

引用

页码：1729 / 1740

页数：12

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