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The Antileukemic Action of Two Thiadiazole Derivatives^*

( Graduate Department of Biochemistry, Brandeis University, Waltham, Mass., and Laboratory of Chemical Pharmacology, National Cancer Institute, Bethesda, Md.)

The thiadiazole derivatives 2-amino-1,3-4-thiadiazole and 2-ethylamino-1,3,4-thiadiazole retarded the growth of leukemia L1210 and extended the survival time of the mice. The thiadiazoles were approximately as effective as the folic acid antagonist aminopterin but considerably less effective than amethopterin in increasing the life span of the leukemic mice.

The antileukemic action and host toxicity of the thiadiazoles were blocked by administration of nicotinamide.

In vitro exchange of thiadiazole with the nicotinamide moiety of DPN was obtained, resulting in the formation of the thiadiazole analog of DPN. C¹⁴-labeled thiadiazole was readily incorporated in the various tissues of the leukemic host.

Preliminary attempts to demonstrate formation of the thiadiazole analog of DPN in vivo were inconclusive.

^* Presented in part at the 49th Annual Meeting of the American Association for Cancer Research, Philadelphia, Pennsylvania, April 11–13, 1958.

Aided by grants from the National Cancer Institute, National Institutes of Health (Grant #NIH CY-3611), and the American Cancer Society, Massachusetts Division. Publication #55 of the Graduate Department of Biochemistry, Brandeis University.

Received 3/10/60.