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Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2002 May 06; Vol. 12 (9), pp. 1269-73. - Publication Year :
- 2002
-
Abstract
- Compound 1 has been shown to be a dual prenylation inhibitor with FPTase (IC50=2 nM) and GGPTase-I (IC50=95 nM). Analogues of 1, which replaced the cyanophenyl group with various biaryls, led to the discovery of highly potent dual FPTase/GGPTase-I inhibitors. 4-trifluoromethylphenyl, trifluoropentynyl, and trifluoropentyl were identified as good p-cyano replacements.
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 12
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 11965368
- Full Text :
- https://doi.org/10.1016/s0960-894x(02)00154-3