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-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.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis; D007942:Leukemia, Experimental / Q000188:drug therapy; D051379:Mice; D011728:Pyridones / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D011728:Pyridones