Pyridones as potential antitumor agents II: 4-Pyridones and bioisosteres of 3-acetoxy-2-pyridone.
Pyridone structural requirements for activity against murine P-388 leukemia have been extended to isosteric analogs of 3-hydroxy-4-pyridone, a compound previously found to have activity. An amino group can be substituted for the 3-hydroxyl function with retention of activity. A sulfur, but not an amino function, can replace the lactam oxygen in the 2-position. Relocation of the lactam oxygen from the 2- to the 4-position in the pyridine ring also produces active pyridones, including 2-methyl-3-acetoxy-4-pyridone. This compound, which has a T/C value of 179%, is the most active material discovered thus far in the pyridone studies.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D007941:Leukemia P388 / Q000188:drug therapy; D051379:Mice; D011728:Pyridones / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D011728:Pyridones; C026751:3-acetoxy-2-pyridone