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New designed EGFR inhibitors (7-11) were prepared from the pyrazolo[3,4-d]pyrimidine intermediates 4a-d including different moieties. All newly synthesized compounds were confirmed by elemental analyses and spectral data. The molecular simulation docking to protein tyrosine kinase (EGFR), using erlotinib (Tarceva TM) as a lead compound was also studied. Some of the prepared compounds were screened for in-vitro cytotoxic activity. The docking results were in coincidence with the biological results that indicated compound 7a showed an inhibitory activity against human breast carcinoma cell line (MCF-7) [IC50 (14.86μM)].