808762-36-9Relevant articles and documents
Synthesis, Biological Activity, and Crystal Structure of N,N-Diethyl-2-{[7-methoxy-4-(phenylamino)quinazolin-6-yl]oxy}acetamide Derivatives
Cai, Zhi-qiang,Han, Xiao,Hou, Ling,Li, Shuai,Wu, Li-hua
, p. 2286 - 2291 (2021/12/23)
Abstract: 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 1H 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.
Synthesis, crystal structure and anticancer activity of substituted quinazoline derivatives
Cai, Zhi-Qiang,Li, Ji-Xin,Li, Shuai,Li, Xiang,Shi, Xiao-Yu,Wang, Bo
, p. 466 - 474 (2021/08/21)
News series of substituted quinazoline derivatives has been synthesized from 3,4-dihydro-7-methoxy-4-oxoquinazoline-6-yl acetate (1) by five-step procedures including chlorination, amination, hydrolysis and etherification. The structures of target compounds were confirmed by IR, 1H-NMR, element analysis and single-crystal X-ray diffraction. The results showed that the compound 8c exhibited remarkable inhibitory activity against MCF-7 cell lines with inhibition rate value of 38.45 %, which was comparable to that of the positive control Gefitinib (inhibition rate = 13.25 % for MCF-7). The initial relationship between structure and activity was worth further exploration.
Phenalene derivatives
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Page 13-14, (2008/06/13)
Novel 1,3,4-triaza-phenalene and 1,3,4,6-tetraazaphenalene derivatives are disclosed. These compounds inhibit epidermal growth factor receptor (“EGFR”) tyrosine kinase. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful, inter alia, in the treatment or control of cancer, in particular solid tumors. This invention also relates to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors.