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Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2005 Jan 03; Vol. 15 (1), pp. 153-8. - Publication Year :
- 2005
-
Abstract
- A non-methionine FT inhibitor lead structure (1) was designed through computer modeling of the peptidomimetic FT inhibitor ABT839. Optimization of this lead resulted in compounds 2e and 2g, with FT IC(50) values of 1.3 and 1.8 nM, GGT IC(50) of 1400 nM, and EC(50) (Ras processing) values of 13 and 11 nM, respectively.
- Subjects :
- Computer Simulation
Farnesyltranstransferase
Imidazoles
Models, Molecular
Molecular Mimicry
Nitriles
Alkyl and Aryl Transferases antagonists & inhibitors
Biphenyl Compounds chemical synthesis
Biphenyl Compounds pharmacology
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors pharmacology
Nicotinic Acids chemical synthesis
Nicotinic Acids pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 15
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 15582430
- Full Text :
- https://doi.org/10.1016/j.bmcl.2004.10.014