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Sun B.,Key Laboratory of Structure based Drug Design & Discovery | Yin X.,Key Laboratory of Structure based Drug Design & Discovery | Zhang J.,Shenyang Pharmaceutical University | Huang J.,Key Laboratory of Structure based Drug Design & Discovery | And 7 more authors.
Chemical Research in Chinese Universities | Year: 2015

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. © 2015, Jilin University, The Editorial Department of Chemical Research in Chinese Universities and Springer-Verlag GmbH. Source

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