Antitumor Effects of biologic Reducing Agents Related to 3,4-Dihydroxybenzylamine: Dihydroxybenzaldehyde, Dihydroxybenzaldoxime, and Dihydroxybenzonitrile

This report describes a structure-activity analysis of isomers of three classes of dihydroxybenzene derivatives, including dihydroxybenzaldoxime, dihydroxybenzaldehyde, and dihydroxybenzonitrile. These derivatives were examined for their effect on ribonucleotide reductase activity, macromolecular sy...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1987-07, Vol.76 (7), p.513-515
Main Authors: Wick, Michael M., Fitzgerald, George B.
Format: Article
Language:English
Subjects:
Animals
Antineoplastic Agents
Benzaldehydes - pharmacology
Biological and medical sciences
Catechols - pharmacology
DNA, Neoplasm - biosynthesis
Dopamine - analogs & derivatives
Dopamine - pharmacology
General pharmacology
Leukemia L1210 - drug therapy
Leukemia L1210 - metabolism
Male
Medical sciences
Mice
Nitriles - pharmacology
Oximes - pharmacology
Pharmacology. Drug treatments
Physicochemical properties. Structure-activity relationships
Ribonucleotide Reductases - antagonists & inhibitors
Structure-Activity Relationship
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Summary:This report describes a structure-activity analysis of isomers of three classes of dihydroxybenzene derivatives, including dihydroxybenzaldoxime, dihydroxybenzaldehyde, and dihydroxybenzonitrile. These derivatives were examined for their effect on ribonucleotide reductase activity, macromolecular synthesis, cell growth, and in vivo antitumor activity against the L1210 murine leukemia. One of the compounds studied exhibited significant antitumor activity against the growth of L1210 leukemia cells. A comparison of the various analogues revealed a possible correlation for 3,4-dihydroxybenzaldoxime between its potent inhibitory effect toward ribonucleotide reductase activity (IC50=38 μM) and its superior L1210 antitumor activity [percent increased life span (% ILS)=100].
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600760704