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.

集落刺激因子-1受体（CSF-1R或FMS）及其配体CSF-1信号调节肿瘤相关巨噬细胞（TAM）的分化和功能，在肿瘤进展中起重要作用。合成了噻吩并[3,2- d ]嘧啶衍生物，并将其评估为FMS的激酶抑制剂。最有代表性的化合物21 对FMS激酶显示出很强的活性（IC ₅₀ = 2 nM），可作为概念验证的候选物。使用人乳腺腺癌细胞通过肿瘤细胞生长抑制测定和体外肿瘤侵袭测定来检查单独和/或与紫杉醇联合的抗肿瘤活性。