| Synthesis and structure-activity relationships study of α-aminophosphonate derivatives containing a quinoline moiety |
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| 作者姓名： | Xi-Feng Zhu Jing Zhang Shuo Sun Yan-Chun Guo Shu-Xia Cao Yu-Fen Zhao |
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| 作者单位： | 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 |
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| 基金项目： | We gratefully acknowledge financial support of this work by the National Natural Science Foundation of China (Nos. 21105091, 21172201). |
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| 摘 要： | Two series of a-aminophosphonate derivatives containing a quinoline moiety have been designed and synthesized by introducing bioactive quinoline scaffold to a-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 2.26 mmol/L–7.46 mmol/L.
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Synthesis and structure-activity relationships study of α-aminophosphonate derivatives containing a quinoline moiety |
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| Xi-Feng Zhu,Jing Zhang,Shuo Sun,Yan-Chun Guo,Shu-Xia Cao,Yu-Fen Zhao.Synthesis and structure-activity relationships study of α-aminophosphonate derivatives containing a quinoline moiety[J].Chinese Chemical Letters,2017,28(7):1514-1518. |
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| Authors: | Xi-Feng Zhu Jing Zhang Shuo Sun Yan-Chun Guo Shu-Xia Cao Yu-Fen Zhao |
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| Institution: | 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 |
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| Abstract: | 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. |
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| Keywords: | Quinoline α-Aminophosphonate Synthesis Antitumor activity In vitro |
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