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■ Synthesis and Biological Activities of Selenium/Thioether Quinazoline Compounds

Canjun Yan, Yuchun Zhang, Guihan Zhao, Xiaohong Jin, Wuwei Yang, Pengpeng Niu, Haojie Wang, and Gang Liu*

*School of Chemistry and Materials Science, Ludong University, Yantai 264025 China

Abstract

In view of the important role of quinazoline skeletons in anti-cancer drugs like Gefitinib and the vital importance of organoselenium compounds in biomedicine field, in this protocol, twenty quinazoline selenium derivatives were designed and synthesized with the aim to develop new anti-cancer drugs by utilizing the synergistic effects of quinazoline skeleton and selenium. In addition, the synthetic method of thioether substituted quinazolines was improved. The biological activities of title compounds were determined against A549 cancer cells in vitro by using MTT assay at 1 μM and 10 μM concentrations. The results showed that most of the title compounds had good anticancer activities. Of note, 6-chloro-4-benzylselenoquinazoline (G5) exhibited better inhibitory activity (67.8% inhibition ratio) than the positive control drug Gefitinib (62.9% inhibition ratio) at the concentration of 10 μM. These findings will provide some clues for further research of anticancer drugs.