Design, Synthesis and Pharmacological Evaluation of Novel 4-Phenoxyquinoline Derivatives as Potential Antitumor Agents
查看参考文献25篇
|
文摘
|
A series of novel 4-phenoxyquinoline derivatives containing 3-amino-2-cyano-acrylamide framework was designed and synthesized, and the in vitro cytotoxic activities of them against five cancer cell lines(HT-29, H460, A549, MKN-45, and U87MG) were evaluated. Most of the compounds exhibited moderate-to-significant cytotoxicity and high selectivity against one or more cell lines as compared with Foretinib. The studies of their preliminary structure-activity relationships(SARs) indicate that the compounds containing methyl groups, especially methyl groups at 4-position of the phenyl ring(moiety B) are more effective. Among them, compound 36 shows the most potent antitumor activities with IC_(50) values of 0.04, 0.09, 0.67, 0.39 and 1.10 μmol/L against HT-29, H460, A549, MKN-45 and U87MG cell lines, respectively. |
|
来源
|
Chemical Research in Chinese Universities
,2015,31(5):746-755 【核心库】
|
|
DOI
|
10.1007/s40242-015-5166-3
|
|
关键词
|
4-Phenoxyquinoline derivative
;
Cytotoxic activity
;
3-Amino-2-cyano-acrylamide
|
|
地址
|
1.
Shenyang Pharmaceutical University, Key Laboratory of Structure-based Drug Design and Discovery, Ministry of Education, Shenyang, 110016
2.
Fujian Institute of Microbiology, Fuzhou, 350007
|
|
语种
|
英文 |
|
文献类型
|
研究性论文 |
|
ISSN
|
1005-9040 |
|
学科
|
化学 |
|
基金
|
Supported by the Program for Liaoning Innovative Research Team in University, China
|
|
文献收藏号
|
CSCD:5537994
|
参考文献 共
25
共2页
|
|
1.
Bottaro D P.
Science,1991,251:802
|
被引
45
次
|
|
|
|
|
2.
Yu H Y.
Chem. J. Chinese. Universitie,2014,35(5):903
|
被引
2
次
|
|
|
|
|
3.
Wang S Y.
Journal of Hepatolog,2004,41:267
|
被引
7
次
|
|
|
|
|
4.
Corso S.
Trends Mol. Med,2005,11:284
|
被引
6
次
|
|
|
|
|
5.
Riccardo F.
Oncogene,1996,12:1697
|
被引
1
次
|
|
|
|
|
6.
Francesca D B.
Cancer Ther,2004,213:317
|
被引
1
次
|
|
|
|
|
7.
Underiner L T.
Anticancer Agent Med,2010,10:7
|
被引
1
次
|
|
|
|
|
8.
Yakes F M.
Mol. Cancer Ther,2011,10:2298
|
被引
33
次
|
|
|
|
|
9.
Kim K S.
J. Med. Chem,2008,51:5330
|
被引
5
次
|
|
|
|
|
10.
Norman M H.
J. Med. Chem,2012,55:1858
|
被引
4
次
|
|
|
|
|
11.
Liu L B.
J. Med. Chem,2012,55:1868
|
被引
3
次
|
|
|
|
|
12.
Zhai X. Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives.
Chem. Res. Chinese. Universities,2013,29(1):62
|
被引
4
次
|
|
|
|
|
13.
Li S.
Eur. J. Med. Chem,2013,64:62
|
被引
1
次
|
|
|
|
|
14.
Qi B H.
Arch. Pharm. Chem. Life Sci,2013,346:596
|
被引
2
次
|
|
|
|
|
15.
Qi B H.
Bioorg. Med. Chem,2013,21:5246
|
被引
5
次
|
|
|
|
|
16.
Li S.
Bioorg. Med. Chem,2013,21:2843
|
被引
11
次
|
|
|
|
|
17.
Li S.
Arch. Pharm. Chem. Life Sci,2013,346:521
|
被引
1
次
|
|
|
|
|
18.
Tang Q D.
Eur. J. Med. Chem,2013,69:77
|
被引
2
次
|
|
|
|
|
19.
Tang Q D.
Bioorg. Med. Chem,2014,22:1236
|
被引
2
次
|
|
|
|
|
20.
Zhou S G.
Bioorg. Med. Chem,2014,22:6438
|
被引
3
次
|
|
|
|
|
了解气象卫星更多信息，请访问