Sinomenine derivatives with embedment of nitrogen-containing heterocycles exhibiting potent TNF-inhibitory activity  

作　　者：WANG Meng MA LiYan LOU YangTong BIAN Chao ZHOU TingTing ZHOU HaiBin LIAO HongZe MA Zhao YIN DongSheng CHEN AiZhong WANG ShaoZhong YANG ZhenYu SUN Bing YAO ZhuJun 

机构地区：[1]State Key Laboratory of Coordination Chemistry and Nanjing National Laboratory of Microstructures,Institute of Chemical Biology and Drug Innovation,School of Chemistry and Chemical Engineering,Nanjing University,Nanjing 210093,China [2]Shanghai Institute of Biochemistry and Cell Biology,Shanghai Institutes of BiologicalSciences,Chinese Academy of Sciences,Shanghai 200031,China [3]State Key Laboratory of Bioorganic and Natural Products Chemistry,Shanghai Institute of Organic Chemistry,Chinese Academy of Sciences,Shanghai 200032,China

出　　处：《Science China Chemistry》2012年第12期2537-2547,共11页中国科学（化学英文版）

基　　金：supported by the National Basic Research Program of China(973 Program,2010CB833200);National Natural Science Foundation of China(90713044,21032002);SHMCST (08431903000);the Fundamental Research Funds for the Central Universities(1082020502)

摘　　要：Inhibitory effect on tumor necrosis factor-c~ （TNF-c0 production by sinomenine derivatives with embedment of small drug-like nitrogen hetereocyclic moieties has been studied in this work. Several new sinomenine derivatives having chlorophenyl sub- stituent have been found to exhibit much more potent TNF-a inhibitory activity than natural sinomenine and other derivatives.Inhibitory effect on tumor necrosis factor-(TNF-) production by sinomenine derivatives with embedment of small drug-like nitrogen hetereocyclic moieties has been studied in this work.Several new sinomenine derivatives having chlorophenyl substituent have been found to exhibit much more potent TNF-α inhibitory activity than natural sinomenine and other derivatives.

关 键 词：SINOMENINE druggability HETEROCYCLE tumor necrosis factor-m inhibition 

分 类 号：Q255[生物学—细胞生物学] TQ457.27[化学工程—农药化工]