Design and synthesis of new EGFR- tyrosine kinase inhibitors containing pyrazolo[3,4-pywmidine cores as anticancer agents

ABSTRACT

New designed EGFR inhibitors [7-1 1] were prepare dfrom the pyrazolo[3t4-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] [1C so [14.86microM]