Pyridones as Potential Antitumor Agents

Based on the finding that 3-acetoxy-2-pyridone had reproducible activity against murine P-388 lymphocytic leukemia, derivatives in this series were synthesized and evaluated to determine structural parameters important for activity. Of the 32 compounds tested, 10 were active. At least two oxygen-con...

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Veröffentlicht in:Journal of pharmaceutical sciences 1979-07, Vol.68 (7), p.816-819
Hauptverfasser: Hwang, Deng Ruey, Driscoll, John S.
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Driscoll, John S.
description Based on the finding that 3-acetoxy-2-pyridone had reproducible activity against murine P-388 lymphocytic leukemia, derivatives in this series were synthesized and evaluated to determine structural parameters important for activity. Of the 32 compounds tested, 10 were active. At least two oxygen-containing functional groups are required for P-388 activity, and the 2,3-isomeric arrangement provides the greatest activity. Carbamate or acyloxy groups in the 3-position produced the most active 2-pyridones.
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subjects Animals
antineoplastic activity
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic agents, potential—pyridone derivatives, structure-activity relationships, mice
Leukemia, Experimental - drug therapy
Mice
potential-pyridone derivatives
Pyridone derivatives-antineoplastic activity
Pyridone derivatives—antineoplastic activity, structure-activity relationships, mice
Pyridones - chemical synthesis
Pyridones - pharmacology
Structure-Activity Relationship
structure-activity relationships
Structured-activity relationships-pyridone derivatives
Structured-activity relationships—pyridone derivatives, antineoplastic activity, mice
title Pyridones as Potential Antitumor Agents
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