Download MendeleyDesign, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors.
Li, Q., Claiborne, A., Li, T., Hasvold, L., Stoll, V.S., Muchmore, S., Jakob, C.G., Gu, W., Cohen, J., Hutchins, C., Frost, D., Rosenberg, S.H., Sham, H.L.(2004) Bioorg Med Chem Lett 14: 5367-5370
- PubMed: 15454228
- DOI: https://doi.org/10.1016/j.bmcl.2004.08.012
- Primary Citation of Related Structures:
1X81 - PubMed Abstract:
As a part of our efforts to identify potent inhibitors of farnesyltransferase (FTase), modification of the structure of tipifarnib through structure-based design was undertaken by replacing the 2-quinolones with 4-quinolones and pyridones, and subsequent relocation of the D-ring to the N-methyl group on the imidazole ring. This study has yielded a novel series of potent and selective FTase inhibitors. The X-ray structure of tipifarnib (1) in complex with FTase was described.
Organizational Affiliation:
Cancer Research, GPRD, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. qun.li@abbott.com
