Effects of nicotinamide and related compounds on the antileukemic activity of 2-amino-1,3,4-thiadiazole.

Paper

Effects of nicotinamide and related compounds on the antileukemic activity of 2-amino-1,3,4-thiadiazole.

Published Dec 1, 1960 · H. Oettgen, J. A. Reppert, V. Coley

Cancer research

Q1 SJR score

12

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0

Influential Citations

Semantic Scholar

Abstract

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.

In Vitro Study

Study Snapshot

Nicotinamide and related compounds effectively reverse the antileukemic activity of 2-amino-1,3,4-thiadiazole against transplanted mouse leukemia B82, indicating that the term "niacin antagonist" encompasses various metabolic activities.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Effects of nicotinamide and related compounds on the antileukemic activity of 2-amino-1,3,4-thiadiazole.

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References

Comparison of teratogenic chemicals in the rat and chick embryos; an exhibit with additions for publication.

Drugs teratogenic in chick embryos may produce consistent developmental abnormalities in rat fetuses, highlighting the need for further studies on maternal protection.

Significance of Enzymatically Catalyzed Exchange Reactions in Chemotherapy

Nicotinamide or DPN protect against acetyl pyridine toxicity in mice, suggesting their importance in chemotherapy.

Application of a Metabolic Inhibitor to the Developing Chick Embryo

3-acetylpyridine injection into the yolk-sac can inhibit chick embryo development and cause mal-development, with limited capacity to convert nicotinic acid to amide.

Production of nicotinic acid deficiency with 3-acetylpyridine, the ketone analogue of nicotinic acid.

3-acetylpyridine can cause nicotinic acid deficiency in mice, similar to the symptoms seen in nicotinic acid-deficient dogs and humans, but the disease disappears when sufficient nicotinic acid or nicotinamide is given.

Citations

2-Amino-1,3,4-thiadiazoles as prospective agents in trypanosomiasis and other parasitoses

2-amino-1,3,4-thiadiazoles show potential as a new class of antiparasitic agents, offering a promising strategy for developing potent antiparasitic drugs.

Indole bearing thiadiazole analogs: synthesis, β-glucuronidase inhibition and molecular docking study

Indole-based thiadiazole derivatives show outstanding -glucuronidase inhibition, with compound 6 being the most potent, and molecular docking studies confirm stronger hydrogen bonding networks with active site residues.

A theoretical study on the structure of 2-amino-1,3,4-thiadiazole and its 5-substituted derivatives in the gas phase, water, THF and DMSO solutions

Isomer A strongly dominates and dictates the structure of 2-amino-1,3,4-thiadiazoles, with no effect from substituted or solvent-related substituents or solvents.

A sensitive method for the determination of residues of N,N'-bis(1,3,4-thiadiazol-2-yl) methanediamine in rice

This sensitive method effectively determines residues of N,N'-bis(1,3,4-thiadiazol-2-yl) methanediamine (II) in rice, with a mean recovery of 85% and a low limit of determination of 0.01 mg kgf.

Mechanism of action of 2,2'-(methylenediimino)bis-1,3,4-thiadiazole (NSC 143019), an antitumor agent.

NSC 143019 inhibits DNA and RNA synthesis without significantly affecting protein synthesis, suggesting its primary action may be due to inhibition of GMP biosynthesis at the step of conversion of IMP to xanthosine 5'-phosphate.