Design, Synthesis and Bioactivities Evaluation of Novel Quinazoline Analogs Containing Oxazole Units. Issue 6 (17th June 2014)

• Record Type: Journal Article
• Authors: Hou, Xuehui; Zhang, Jingyu; Zhao, Xuan; Chang, Liming; Hu, Ping; Liu, Hongmin
• Is Part Of: Chinese journal of chemistry. Volume 32:Issue 6(2014:Jun.)
• Page Start: 538
• Page End: 544
• Publication Date: 2014-06-17
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1002/cjoc.201400271
• Languages: English
• ISSNs: 1001-604X

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>A novel type of quinazoline derivatives, which were designed by the combination of quinazoline as the backbone and oxazole scaffold as the substituent, have been synthesized and their biological activities were evaluated for anti‐proliferative activities and EGFR inhibitory potency. Compound <bold>12b</bold> demonstrated the most potent inhibitory activity (IC₅₀=0.95 µmol/L for EGFR), which could be optimized as a potential EGFR inhibitor in the further study. The structures of the synthesized quinazoline analogs and all intermediates were comfirmed by ¹H and ¹³C NMR, 2D NMR spectra, IR spectra and MS spectra.</p> </abstract>