Design, synthesis and biological evaluation of a novel series of 1,3,4-oxadiazole bearing N-methyl-4-(trifluoromethyl)phenyl pyrazole moiety as cytotoxic agents

被引：102
|
作者：
Puthiyapurayil, Pushpan [1 ,2 ]
Poojary, Boja [1 ]
Chikkanna, Chandrashekhar [3 ]
Buridipad, Sunil Kumar [4 ]
机构：
[1] Mangalore Univ, Dept Chem, Mangalagangothri 574199, Karnataka, India
[2] Syngene Int Ltd, Bangalore 560099, Karnataka, India
[3] SDM Coll, Dept Med Chem, Dk 574342, Karnataka, India
[4] NET Pharm Coll, Dept Pharm Coll, Raichur 584103, Karnataka, India
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 53卷
关键词：
N-Methyl-4(trifluoromethyl)phenyl; Pyrazole; Cytotoxic activity; MTT assay; Doxorubicin; Nuclear overhauser effect; ANTITUMOR-ACTIVITY; IN-VITRO; DERIVATIVES; INHIBITORS; IDENTIFICATION; ANALOGS; ETHERS;
D O I：
10.1016/j.ejmech.2012.03.056
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
On account of the reported anticancer activity of pyrazoles and oxadiazoles, we have designed and synthesized a novel combinatorial library of S-substituted-1,3,4-oxadiazole bearing N-methyl-4-(trifluoromethyl)phenyl pyrazole moiety and tested for in-vitro cytotoxic activity by MTT assay. Amongst the tested compounds, the compound 5e was the most promising anticancer agent with IC50 value of 15.54 mu M in MCF-7 cells, compared to Doxorubicin as standard drug. The newly synthesized compounds were characterized by NOE, IR, H-1 NMR, C-13 NMR and LC-MS analysis. (C) 2012 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：203 / 210
页数：8
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