Citation: Zhu Xi-Feng, Zhang Jing, Sun Shuo, Guo Yan-Chun, Cao Shu-Xia, Zhao Yu-Fen. Synthesis and structure-activity relationships study of α-aminophosphonate derivatives containing a quinoline moiety[J]. Chinese Chemical Letters, ;2017, 28(7): 1514-1518. doi: 10.1016/j.cclet.2017.02.012 shu

Synthesis and structure-activity relationships study of α-aminophosphonate derivatives containing a quinoline moiety

Zhu Xi-Feng ^a ,
Zhang Jing ^a ,
Sun Shuo ^b ,
Guo Yan-Chun ^a,, ,
Cao Shu-Xia ^a,, ,
Zhao Yu-Fen ^a,c

a.
The College of Chemistry and Molecular Engineering, The Key Laboratory of Chemical Biology and Organic Chemistry of Henan Province, Zhengzhou University, Zhengzhou 450001, China
b.
Department of Chemistry, International College of Zhengzhou University, Zhengzhou University, Zhengzhou 450001, China
c.
Department of Chemistry, College of Chemistry and Chemical Engineering, The Key Laboratory for Chemical Biology of Fujian Province, Xiamen University, Xiamen 361005, China

Corresponding author: Guo Yan-Chun, ycguo@zzu.edu.cn Cao Shu-Xia, csx@zzu.edu.cn
Received Date: 8 October 2016
Revised Date: 11 December 2016
Accepted Date: 27 December 2016
Available Online: 20 July 2017

Figures(2)

Two series of α-aminophosphonate derivatives containing a quinoline moiety have been designed and synthesized by introducing bioactive quinoline scaffold to α-aminophosphonate. The in vitro cytotoxic activities of target compounds were first investigated against two human cancer cell lines including Eca109 and Huh7 by MTT assay. Results revealed that most of target compounds exhibited moderate to high antitumor activities against the tested cancer cell lines and some demonstrated more potent inhibitory activities compared with Sunitinib. Among them, compounds 4b2 and 4b4 containing methylsubstituted aniline group were found to be more active than Sunitinib against both of two cancer cell lines, with IC₅₀ in the range of 2.26μmol/L-7.46μmol/L.
- Quinoline,
- α-Aminophosphonate,
- Synthesis,
- Antitumor activity,
- In vitro
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