Abstract
Based on the molecular docking studies, which were performed to position Erlotinib and the target compounds into the active site of the epidermal growth factor receptor(EGFR) to determine the probable binding model, a novel series of 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine derivatives as the novel potential EGFR kinase inhibitors was designed and synthesized. The antitumor activity of all the target compounds against human pulmonary carcinoma cell line A549 has been screened. Of all the target compounds, 4-[2-(1-piperidyl)carbonylmethoxylphenthio]- 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine(7j) demonstrated the most potent antitumor activity. Several of the target compounds exhibited moderate antitumor activity. The preliminary structure-activity relationships of some target compounds were summarized.
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Supported by the National Natural Science Foundation of China(No.21342006) and the Program for the Innovative Research Team of the Ministry of Education of China(No.IRT_14R36).
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Sun, B., Yin, X., Zhang, J. et al. Synthesis, characterization and biological activity of tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine derivatives as epidermal growth factor receptor inhibitors. Chem. Res. Chin. Univ. 31, 936–941 (2015). https://doi.org/10.1007/s40242-015-5202-3
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DOI: https://doi.org/10.1007/s40242-015-5202-3