Synthesis of 5-substituted benzyl-2,4-diamino pyrimidine derivatives as c-Fms kinase inhibitors  

作　　者：Li Bao Xu Wei Sun Hong Ying Liu Li Li Wang Jun Hai Xiao Xiao Hong Yang Song Li 

机构地区：[1]School of Pharmaceutical Sciences, Jilin University, Changchun 130021, China [2]Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China

出　　处：《Chinese Chemical Letters》2010年第11期1318-1321,共4页中国化学快报（英文版）

基　　金：financially supported by the National High-Tech Research and Development Program of China(863 Program)(No.2006AA10A201);National Natural Science Foundation(No.30472093)

摘　　要：A serials of novel 5-substituted benzyl-2,4-diamino pyrimidine derivatives have been synthesized and evaluated as inhibitors of c-Fms kinase by the standard MTT method.The results showed that compound 15,5-[3-methoxy-4-（pyridine-3-yl）benzyl]-2,4-diamino pyrimidine,had an IC50 of 1.45μmol/L in inhibiting the proliferation of M-CSF-dependent myeloid leukemia cells in mice （NFS-60）,which was similar with GW2580,a selective inhibitor of c-Fms kinase.A serials of novel 5-substituted benzyl-2,4-diamino pyrimidine derivatives have been synthesized and evaluated as inhibitors of c-Fms kinase by the standard MTT method.The results showed that compound 15,5-[3-methoxy-4-（pyridine-3-yl）benzyl]-2,4-diamino pyrimidine,had an IC50 of 1.45μmol/L in inhibiting the proliferation of M-CSF-dependent myeloid leukemia cells in mice （NFS-60）,which was similar with GW2580,a selective inhibitor of c-Fms kinase.

关 键 词：C-Fms kinase inhibitors Synthesis 2 4-Diamino pyrimidine 

分 类 号：TQ457.29[化学工程—农药化工] S831.5[农业科学—畜牧学]