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

作     者：Xi-Feng Zhu Jing Zhang Shuo Sun Yan-Chun Guo Shu-Xia Cao Yu-Fen Zhao 

作者机构：The College of Chemistry and Molecular EngineeringThe Key Laboratory of Chemical Biology and Organic Chemistry of Henan ProvinceZhengzhou UniversityZhengzhou 450001China Department of ChemistryInternational College of Zhengzhou UniversityZhengzhou UniversityZhengzhou 450001China Department of ChemistryCollege of Chemistry and Chemical EngineeringThe Key Laboratory for Chemical Biology of Fujian ProvinceXiamen University Xiamen 361005China 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2017年第28卷第7期

页      面：1514-1518页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 10[医学] 

基　　金：financial support of this work by the National Natural Science Foundation of China(Nos.21105091 21172201) 

主　　题：Quinoline a Aminophosphonate Synthesis Antitumor activity In vitro 

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.