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Effects of Nicotinamide and Related Compounds on the Antileukemic Activity of 2-Amino-1,3,4-thiadiazole^*

( Divisions of Experimental and Clinical Chemotherapy, Sloan-Kettering Institute for Cancer Research; and Cornell University Medical College, New York, N.Y.)

The effect of nicotinamide and a variety of nicotinamide analogs and related compounds on the activity of 2-amino-1,3,4-thiadiazole against transplanted mouse leukemia B82 has been tested. 5-Fluoronicotinamide, 6-aminonicotinamide, N-hydroxy-bis-methylnicotinamide, N-N'-methylene-bis-nicotinamide, DPN, and 3-acetylpyridine were as potent as nicotinamide and nicotinic acid in reversing the thiadiazole effect. Other nicotinamide analogs, the analogs of nicotinic acid, precursors and catabolic products of nicotinamide have not shown such activity. The results of this study have been compared with results obtained by another author in a different system. It has been concluded that the term "niacin antagonist" represents several different metabolic activities, all reversible by niacin.

^* This investigation was supported in part by research grant CY-3192 from the National Cancer Institute, research contract SA-43-ph-2445 from the Cancer Chemotherapy National Service Center, and by a grant from the American Cancer Society.

Received 6/22/60.