異項環酸と異項環塩基を縮合した酸アミド型化合物の合成とその制癌作用の検討

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By the fusion method, 16 kinds of amide-type compounds were synthesized from the phenyl esters of heterocyclic acids and heterocyclic amines, and their antitumor activities were examined with Ehrlich ascites carcinoma and Crocker sarcoma-180 in mice. None of them had a strong antitumor activity, but 7 of the test compounds, 2-isonicotinoylamino-1,3,4-thiadiazole (VIII), 2-nicotinoylamino-5-isopropyl-1,3,4-thiadiazole (IX), 2-isonico-tinoylamino-5-isopropyl-1,3,4-thiadiazole (X), 2-(α-thenoylamino)-5-isopropyl-1,3,4-thiadiazole (XI), 2-(α-furoylamino)-5-isopropyl-1,3,4-thiadiazole (XII), 2-isonicotinoylamino-5-isobutyl-1,3,4-thiadiazole (XIV), and 2-(α-furoylamino)-5-isobutyl-1,3,4-thiadiazole (XVI), had a moderate to slight antitumor activity against these solid tumors. It was noteworthey that all these effective compounds were the derivatives of 2-amino-1,3,4-thiadiazole.
社団法人日本薬学会の論文
1976-04-25