Solid-phase synthesis of novel inhibitors of farnesyl transferase

Authors
Barber, AM Hardcastle, IR Rowlands, MG Nutley, BP Marriott, JH Jarman, M
Citation
Am. Barber et al., Solid-phase synthesis of novel inhibitors of farnesyl transferase, BIOORG MED, 9(4), 1999, pp. 623-626
Citations number
14
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
4
Year of publication
1999
Pages
623 - 626
Database
ISI
SICI code
0960-894X(19990222)9:4<623:SSONIO>2.0.ZU;2-2
Abstract
A novel diphosphate mimic, the 2,3,6-trifluoro-5-hydroxy-4-nitrophenoxy gro up (1), has been employed as the template in the solid-phase synthesis of n ovel Farnesyl Transferase inhibitors using the Mitsunobu reaction. The most potent inhibitor (farnesyloxy-5-hydroxy-2,3,6-trifluoro-4-nitrobenzene) di splayed an IC50 of 6.3 mu M versus Farnesyl Transferase. (C) 1999 Elsevier Science Ltd. All rights reserved.