ANTI-TUMOR ACTIVITIES OF NEWLY SYNTHESIZED 5-CARBAMOYL-1 H-IMIDAZOL-4YL 1-ADAMANTANECARBOXYLATE AND 5-CARBAMOYL-1 H-IMIDAZOL-4YL PIPERONYLATE

  • 1 January 1980
    • journal article
    • research article
    • Vol. 40  (10) , 3810-3814
Abstract
In synthetic studies on the chemical modification of the nucleoside antibiotic bredinin, 2 new derivatives, 5-carbamoyl-1H-imidazol-4-yl 1-adamantanecarboxylate and 5-carbamoyl-1-imidazol-4-yl piperonylate, possessed a potent antitumor activity in several experimental tumor systems, even though bredinin itself shows only in vitro cytotoxicity and lacks therapeutic effectiveness. These 2 derivatives of bredinin exhibited antitumor activity against a wide variety of tumors, including [mouse] leukemias L1210 and P388 cells, [mouse] Lewis lung carcinoma cells, [mouse] B16 melanoma cells, [mouse] Colon 26 and 38 adenocarcinomas cells, [mouse] Ehrlich carcinoma cells and [mouse] sarcoma 180 cells. These agents showed good therapeutic effects against ascitic types of tumors and against a number of slow-growing solid tumor lines, particularly the ascitic and solid forms of Ehrlich carcinoma. At their optimal doses, both compounds effected a complete cure of all or most of the mice treated. Although the mechanisms of action of these compounds remain unknown, they are able to suppress in vivo tumor growth, presumably by being slowly anabolized in vivo to an active form and inhibiting purine de novo synthesis as bredinin does.

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