Chinese Journal of Organic Chemistry >
Syntheses and in vitro Antitumor Activities of N-Acetyl Pyrazolines and Diphenyl Etheryl N-Acetyl Bis-pyrazolines
Received date: 2015-03-31
Revised date: 2015-05-06
Online published: 2015-05-26
Supported by
Project supported by the Natural Science Foundation of Gansu Province (No. 2014GS03265).
Seven N-acetyl pyrazolines 2a~2g and seven N-acetyl bis-pyrazolines 4a~4g with diphenyl etheryl moiety were synthesized and characterized by 1H NMR,13C NMR, elemental analysis and ESI-MS, and their in vitro antitumor activities on A549, H1299 and MCF-7 were evaluated by 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl-2H-tetrazolium) (MTS) assay. The results showed those compounds exhibited potent antiproliferative effects on cancer cells, among them compound 3,3'-(4,4'-diphenyl ether)-5,5'-bi[1-acetyl-5-(benzo[d][1,3]dioxo-5-yl)-2-pyrazoline] (4e) showed significantly inhibited the growth of all three kinds of cancer cells, the IC50 values of A549, H1299 and MCF-7 were 16.91, 10.09, 10.97 μmol/L, respectively.
Key words： N-acetyl pyrazoline; N-acetyl bis-pyrazoline; diphenyl ether; antitumor
Zhang Yingpeng , Tan Wei , Yang Yunshang , Sun Shiqi , Guo Huichen . Syntheses and in vitro Antitumor Activities of N-Acetyl Pyrazolines and Diphenyl Etheryl N-Acetyl Bis-pyrazolines[J]. Chinese Journal of Organic Chemistry, 2015 , 35(9) : 1985 -1990 . DOI: 10.6023/cjoc201503034
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