Abstract

The reaction of 5‐amino‐3‐methylisoxazole (1) with formalin and secondary amines gave the corresponding Mannich bases 3, 4, 5, 6. Alkylation of isoxazole derivative 1 with Mannich bases hydrochloride gave unsubstituted isoxazolo[5,4‐b]pyridine derivatives 8a, 8b via alkylation at position 4. Moreover, coupling reaction of 1 with different diazonium salts gave the corresponding mono and bisazo dyes of isoxazole derivative. The newly synthesized compounds were screened for their antitumor activity compared with 5‐fluorouracil as a well‐known cytotoxic agent using Ehrlich ascites carcinoma cells. Interestingly, the obtained results showed clearly that compounds 3, 15, 8b, 4, 8a, and 5 exhibited high antitumor activity than 5‐fluorouracil.

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