FACILE AND CONVENIENT SYNTHESIS OF NEW ISOXAZOLO5,4-bPYRIDINE, PYRROLO3,2-dISOXAZOLE, ISOXAZOLO5,4-bAZEPINE-4,7-DIONE AND ISOXAZOLE DERIVATIVES WITH POTENTIAL ANTICANCER ACTIVITY

摘要

The readily available 3-methylisoxazol-5-amine (1) has been used as a key intermediate for the synthesis of isoxazolo5,4-bpyridine, pyrrolo3,2-disoxazole, isoxazolo5,4-bazepine-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, pyrrolo3,2-disoxazole 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.