Synthesis, Biological Activity, and Crystal Structure of N,N-Diethyl-2-{7-methoxy-4-(phenylamino)quinazolin-6-yloxy}acetamide Derivatives

摘要

A number of novel 4-aminoquinazoline derivatives has been synthesized by four-step synthesis. Structures of the synthesized compounds have been characterized by IR and H-1 NMR spectra, element analysis, and single crystal X-ray diffraction. Biological activity of the products has been tested and most of those are characterized by potential antitumor activity against MKN45 cell line. Two compounds exhibit significant inhibitory activity higher than that of Gefitinib used as the positive control. Preliminary structure-activity relationship is considered.