Design synthesis and in vitro antitumor activity evaluation of novel 4-pyrrylamino quinazoline derivatives

摘要

Here we describe the design and synthesis of two series of 4-pyrrylamino quinazolines as new analogues of the EGFR inhibitor Gefitinib. In vitro antitumor activity of these novel compounds against pancreatic (Miapaca2) and prostate (DU145) cancer cell lines was evaluated. Compared with the parental Gefitinib, all the 18 derivatives show a greatly increased cytotoxicity to cancer cells. In vitro kinase inhibitory activity on EGFR was also investigated. Among them, compounds >GI-6, GII-4, GII-6, GII-8, and >GII-9 are more potential RTK inhibitors. Based on these results, we propose simple structure-activity relationship to provide information for designing and developing more potent antitumor agents.