期刊
BIOORGANIC CHEMISTRY
卷 92, 期 -, 页码 -出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2019.103218
关键词
Benzoxazole; Benzimidazole; Cytotoxicity; COXs; Antioxidant
资金
- Jouf university
To enhance the cytotoxicity of benzimidazole and/or benzoxazole core, the benzimidazole/benzoxazole azopyrimidine were synthesized through diazo-coupling of 3-aminophenybenzimidazole (6a) or 3-aminophenylbenzoxazole (6b) with diethyl malonate. The new azo-molanates 6a&b mixed with urea in sodium ethoxide to afford the benzimidazolo/benzoxazolopyrimidine 7a&b. The structure elucidation of new synthesized targets was proved using spectroscopic techniques NMR, IR and elemental analysis. The cytoxicity screening had been carried out against five cancer cell lines: prostate cancer (PC-3), lung cancer (A-549), breast cancer (MCF-7), pancreas cancer (PaCa-2) and colon cancer (HT-29). Furthermore, the antioxidant activity, phospholipase A2-V and cyclooxygenases inhibitory activities of the target compounds 7 aRrb were evaluated and the new compounds showed potent activity (cytotoxicity IC50 range from 4.3 to 9.2 mu m, antioxidant activity from 40% to 80%, COXs or LOX inhibitory activity from 1.92 mu M to 8.21 mu M). The docking of 7a&b was made to confirm the mechanism of action.
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