Citation: Li Bao Xu, Wei Sun, Hong Ying Liu, Li Li Wang, Jun Hai Xiao, Xiao Hong Yang, Song Li. Synthesis of 5-substituted benzy 1-2,4-diamino pyrimidine derivatives as c-Fms kinase inhibitors[J]. Chinese Chemical Letters, ;2010, 21(11): 1318-1321. doi: 10.1016/j.cclet.2010.06.023 shu

Synthesis of 5-substituted benzy 1-2,4-diamino pyrimidine derivatives as c-Fms kinase inhibitors

a School of Pharmaceutical Sciences, Jilin University, Changchun 130021, China;
b Laboratory of Computer-Aided Drug Design & Discovery, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China

Received Date: 23 March 2010

Fund Project: This work was financially supported by the National High-Tech Research and Development Program of China (863 Program)(No.2006AA10A201) and National Natural Science Foundation (No.30472093).

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 1.45 μmol/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.
- C-Fms kinase inhibitors,
- Synthesis,
- 2,4-Diamino pyrimidine
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