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  • Title: Synthesis and evaluation of thieno[3,2-d]pyrimidine derivatives as novel FMS inhibitors.
    Author: Kim YY, Choi J, Choi K, Park C, Kim YH, Suh KH, Ham YJ, Jang SY, Lee KH, Hwang KW.
    Journal: Bioorg Med Chem Lett; 2019 Jan 15; 29(2):271-275. PubMed ID: 30522957.
    Abstract:
    Colony stimulating factor-1 receptor (CSF-1R or FMS) and it ligand, CSF-1, signaling regulates the differentiation and function of tumor-associated macrophages (TAMs) that play an important role in tumor progression. Derivatives of thieno[3,2-d]pyrimidine were synthesized and evaluated as kinase inhibitors of FMS. The most representative compound 21 showed strong activity (IC50 = 2 nM) against FMS kinase and served as candidate for proof of concept. Anti-tumor activity alone and/or in combination with paclitaxel was examined via a tumor cell growth inhibition assay and via an in vitro tumor invasion assay using human breast adenocarcinoma cells.
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