Pyridones as potential antitumor agents II: 4-Pyridones and bioisosteres of 3-acetoxy-2-pyridone.

Abstract

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.

• Authors: D R Hwang, G R Proctor, J S Driscoll
• Journal: Journal of pharmaceutical sciences (J Pharm Sci) Vol. 69 Issue 9 Pg. 1074-6 (Sep 1980) ISSN: 0022-3549 [Print] United States
• PMID: 7411412 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Antineoplastic Agents
• Pyridones
• 3-acetoxy-2-pyridone

Topics

• Animals
• Antineoplastic Agents (chemical synthesis, pharmacology)
• Leukemia P388 (drug therapy)
• Mice
• Pyridones (chemical synthesis, pharmacology)
• Structure-Activity Relationship