Synthesis and in vitro biological evaluation of new pyrazole chalcones and heterocyclic diamides as potential anticancer agents

被引:76
|
作者
Rai, Sankappa U. [1 ]
Isloor, A. M. [2 ]
Shetty, P. [3 ]
Pai, K. S. R. [4 ]
Fun, H. K. [5 ]
机构
[1] Manipal Univ, Manipal Inst Technol, Dept Chem, Manipal, Karnataka, India
[2] Natl Inst Technol Karnataka, Dept Chem, Med Chem Lab, Surathkal 575025, India
[3] Manipal Univ, Manipal Inst Technol, Dept Printing, Manipal, Karnataka, India
[4] Manipal Univ, Manipal Coll Pharmaceut Sci, Dept Pharmacol, Manipal 576104, Karnataka, India
[5] King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia
关键词
MCF; 7; HeLa; EDCI; HOBt; Diamide; BIS-NAPHTHALIMIDE; ANTITUMOR; DNA; BINDING; DERIVATIVES; DISCOVERY; DESIGN;
D O I
10.1016/j.arabjc.2014.01.018
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Synthesis and characterization of new heterocyclic pyrazole chalcones (4a-e) and diamide (6a-e) derivatives are described. Pyrazole chalcones were synthesized by the reaction of pyrazole aldehydes and suitable aromatic ketones. Diamides were synthesized by the reaction of phthalic acid and amines. Newly synthesized compounds were characterized by spectral studies and their biological activity was assessed in vitro using MCF-7 (human breast adenocarcinoma) and HeLa (human cervical tumor cells) cell lines. Few of the synthesized molecules inhibited the growth of the human breast cancer cell lines and human cervical tumor cell lines at low micromolar to nanomolar concentrations. (C) 2014 King Saud University. Production and hosting by Elsevier B.V. All rights reserved.
引用
收藏
页码:317 / 321
页数:5
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