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Paper | Regular issue | Vol 100, No. 6, 2020, pp.901-915
Published online, 10th April, 2020
DOI: 10.3987/COM-20-14245
Facile and Convenient Synthesis of New Isoxazolo[5,4-b]pyridine, Pyrrolo[3,2-d]isoxazole, Isoxazolo[5,4-b]azepine-4,7-dione and Isoxazole Derivatives with Potential Anticancer Activity

Ahmed El-Mekabaty* and Mona E. Ibrahim

*Chemistry Department, Faculty of Science, Mansoura University, El-Gomhoria Street, ET-35516 Mansoura, Egypt


The readily available 3-methylisoxazol-5-amine (1) has been used as a key intermediate for the synthesis of isoxazolo[5,4-b]pyridine, pyrrolo[3,2-d]isoxazole, isoxazolo[5,4-b]azepine-4,7-dione and isoxazole derivatives via its reactions with some chemical reagents. Sixteen compounds were designed to study their cytotoxic properties against three human cell lines: colorectal carcinoma (HCT-116), prostate cancer (PC3) and normal lung fibroblast (WI-38), using the MTT colorimetric assay. 5-Fluorouracil, a well-known anticancer drug, was used for comparison. Among the tested candidates, pyrrolo[3,2-d]isoxazole 5 and isoxazole derivatives 11-14 showed the highest activity against the tested cancer cell lines with good selectivity by their lower toxicity against normal cells.