Studies on Nucleic Acid Antagonists. II. Structure-Activity Relationship in 5-Phenylazopyrimidines.

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Among the 5-phenylazopyrimidine derivatives reported in the preceding paper, some members showed a remarkable inhibitory effect upon the growth of Lactobacillus casei, Tetrahymena geleii, as well as chick embyro fibroblast. Others which were only slightly effective, had anti-tumor activity against Yoshida sarcoma and Ehrlich carcinoma. As a result of study on the structure-activity relationships in these compounds, it was found that 2,4,6-triamino-5-phenylazopyrimidines, in which the para-position of the benzene ring of the 5-phenylazogroup was substituted with sulfonic acid, sulfonamide, carboxylic acid, or phosphonic acid group, were effective upon several transplantable tumors in experimental animals and their anti-tumor activity increased by a combined administration with other nucleic acid antagonists such as 6-mercaptopurine.
社団法人日本薬学会の論文
1959-02-10