Design,synthesis and biological evaluation of new rhodacyanine analogues as potential antitumor agents

作     者：Yang Xiong Li Xin Zhai Wei Ke Liao Wu Fu Zhu Ying He Ping Gong Yang Xiong Li;Xin Zhai;Wei Ke Liao;Wu Fu Zhu;Ying He;Ping Gong

作者机构：Key Laboratory of Structure-based Drug Design and Discovery of Ministry of EducationSchool of Pharmaceutical EngineeringShenyang Pharmaceutieal UniversityShenyang 110016China 

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

年 卷 期：2012年第23卷第4期

页      面：415-418页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 083002[工学-环境工程] 100705[医学-微生物与生化药学] 0830[工学-环境科学与工程（可授工学、理学、农学学位）] 07[理学] 08[工学] 0713[理学-生态学] 10[医学] 

主　　题：Rhodacyanine analogues Antitumor Synthesis 

摘      要：In an attempt to develop potent antitumor agents,new rhodacyanine analogues containing the pyridinium ring（5a-5h）,the isoquinolinium ring（6a-6c） and the quinolinium ring（7a-7e） linked to the rhodanine ring via N-N covalent bond were designed, synthesized and evaluated for antitumor activity against human lung cancer cell line（H460） by MTT assay in *** of the tested compounds showed enhanced antitumor activity with IC_（50） values ranging from 0.006 to 9.2 u,mol/L as compared to the lead compound *** them,the most promising compound 7d（IC_（50） = 0.006μmol/L） was 216.7 times more active than MKT-077（IC_（50） = 1.3μmol/L）.The preliminary structure-activity relationship of the target compounds was discussed.