期刊
TETRAHEDRON
卷 98, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2021.132426
关键词
Aldehyde; Amine; Cytotoxicity; Heterocycle; Iodine; Microwave; One pot synthesis; 4(3H)-Quinazolinones
资金
- Vietnam National Foundation for Science and Technology Development (NAFOSTED) [104.01e2018.51]
- Ministry of Education, Culture, Sports, Science and Technology, Japan (JSPS KAKENHI Grant) [JP19H04649]
In this study, twenty novel quinazolin-4(3H)-one derivatives were synthesized and several compounds were found to possess cytotoxic activities against MCF-7 and A549 cells based on cell viability assays.
Twenty 2,3-disubstituted quinazolin-4(3H)-one derivatives 1-20 were successfully synthesized in moderate to good yields (25-82%). Their syntheses were based on a one pot tandem ring opening procedure followed by iodine-catalyzed oxidative cyclization of isatoic anhydride with aldehydes, using water as the only solvent under both classical and microwave irradiation conditions. Cytotoxicity assays of the prepared compounds against three human cancer cell lines (HeLa, MCF-7, and A549) indicated that 2, 3, and 20 possessed moderate activities against MCF-7 cells (IC50 = 47.2 mu M, 43.9 mu M, and 44.9 mu M, respectively). Good cytotoxic activities against A549 cells were observed for 3 and 8 with IC50 values of 30.7 mu M and 29.8 mu M, respectively, which were comparable to the positive control, 5-fluorouracil (5-FU, IC50 = 27.9 mu M). Furthermore, compound 4 exhibited slightly stronger activity (IC50 = 23.6 mu M) than the positive control 5-FU against the A549 cell line. (C) 2021 Elsevier Ltd. All rights reserved.
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