Cancer is a main reason for human morbidity and mortality globally. Screening and identifying new anticancer chemical substances is considered as a valid treatment for carcinoma. In our study on synthesis and search towards the development of potential anticancer agents, a series of thieno[2,3-d]pyrimidine derivatives were prepared from the functionalized iminophosphorane via aza-Wittig reaction. Their structures were confirmed by 1 H NMR, 13 C NMR, MS and elemental analysis. The in vitro antitumor activities of compounds were analyzed with CCK8 standard method. It revealed these thieno[2,3-d]pyrimi-dine derivatives were exhibited cytotoxicity against HepG2, HEp-2, and MCF-7 cell lines. The most potent compounds, 5 h and 5 j, were efficacious against HEp-2 cells with IC 50 1.8μmol/L and 0.8μmol/L, respectively. Meanwhile, 5 a, 5 d and 5 h showed broad spectrum of cytotoxicity for HepG2, Hep2 and MCF-7 three different cell lines with IC 50 range of 1.8-87.5μmol/L. Furthermore, we demonstrated that cytotoxicity of 5 j was due to the activation of caspase-9 involved apoptotic pathway, which is death receptor independent.

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