1313409-07-2Relevant articles and documents
Synthesis and evaluation of thieno[3,2-d]pyrimidine derivatives as novel FMS inhibitors
Kim, Yu-Yon,Choi, Jaeyul,Choi, Kyungjin,Park, Changhee,Kim, Young Hoon,Suh, Kwee Hyun,Ham, Young Jin,Jang, Sun Young,Lee, Kyu-Hang,Hwang, Kwang Woo
, p. 271 - 275 (2019)
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.