Citation
Ce. O'Connell et al., Synthesis and evaluation of hydroxyproline-derived isoprenyltransferase inhibitors, BIOORG MED, 9(14), 1999, pp. 2095-2100
Citations number
24
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X
→ ACNP
Volume
9
Issue
14
Year of publication
1999
Pages
2095 - 2100
Database
ISI
SICI code
0960-894X(19990719)9:14<2095:SAEOHI>2.0.ZU;2-2
Abstract
A series of peptidomimetics based on a hydroxyproline scaffold was prepared
and evaluated for inhibition of farnesyltransferase and geranylgeranyltran
sferase I in both enzymatic and cell-based assays. A number of analogs were
potent and selective inhibitors of FTase, while one compound (22) was nons
elective in the enzymatic assays but eight-fold selective for inhibition of
GGTase in the cellular assay (IC50 = 0.39 mu M) (C) 1999 Elsevier Science
Ltd. All rights reserved.