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：104

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

页码：203 / 210

页数：8

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