A number of derivatives of isoxazolo [4,3-d]pyrimidine and isoxazolo [4,5-d]pyrimidine were prepared with potential anticancer activity. Condensation of 4-amino-5-benzoyl-isoxazolo-3-carboxylic acid hydrazide with ethyl orthoformate and then with different amines gave a series of 3-benzoyl-7-oxo-7H-isoxazolo[4,3-d]pyrimidin-6-yl-aryliden-formamidine. A series of 5-aminomethyl-7-phenyl-isoxazolo[4,5-d]pyrimidine-3-carboxamide was obtained from 4-amino-5-benzoylisoxazole-3-carboxamide with acetonitrile, and chloroacetonitrile with gaseous hydrogen chloride. Some of these compounds were tested for their cytotoxic activity.
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Fused pyrimidine derivatives R 0515 Synthesis and Pharmacological Screening of Derivatives of Isoxazolo[4,5-d]pyrimidine. -Starting from compound (I) a number of heterocycles is prepared. Compounds (IV), (VII), (IX), (XI), and (XII) are tested for their anticancer activity; only (IV) shows interesting activity on a panel of 62 tumor cell lines. Derivatives (IXa) and (XIIb) are tested for their effects on the immune response in the mouse model. The results indicate that (XIIb) is a universal inhibitor of the immune response, while (IXa) selectively suppresses the humoral immune response. -(WAGNER*, E.; AL-KADASI, K.; ZIMECKI, M.; SAWKA-DOBROWOLSKA, W.; Eur.
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