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

被引:14
|
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
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
收藏
页码:1729 / 1740
页数:12
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