The derivatives of isoxazolopyridine have interesting biological properties. These compounds showed bacteriostatic, analgesic, anti-inflammatory, cardiotonic and hypotensive, myolytic, antilipidemic and anxiolytic activity. Two of these derivatives were investigated in clinical studies: THIP  and THOPO as agonist GABA-receptors are used as anxiolytic agents. Herein, The synthesis of a new series isoxazolo[4,5-b]pyridines is described. 4-Amino-5-benzoyl-  3-carbamoylisoxazol was subjected to reactions with selected active methylene compounds in the polar solvent or in the presence of ZnCl₂ or In(OTf)₃ (under solvent-free conditions), leading to the production of the diverse substituted isoxazolo[4,5-b]pyridines in good yields. The chosen compounds were examined for antiproliferative activity in vitro against 8 various human or mouse cancer lines, using SRB technique. Two of them: revealed cytotoxic activity against the cells of all human tumor cell lines applied. Moreover, their ID₅₀ values are in the range of the international activity criterion for synthetic agents (4 mg/ml).

1. POSTER: Catalytic synthesis and antiproliferative activity in vitro of polisubstituted isoxazolopyridine derivatives., Microsoft Office Document, 0MB

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