Potent inhibitors of protein farnesyltransferase: Heteroarenes as cysteinereplacements

Authors
Shen, W Fakhoury, S Donner, G Henry, K Lee, J Zhang, HC Cohen, J Warner, R Saeed, B Cherian, S Tahir, S Kovar, P Bauch, J Ng, SC Marsh, K Sham, H Rosenberg, S
Citation
W. Shen et al., Potent inhibitors of protein farnesyltransferase: Heteroarenes as cysteinereplacements, BIOORG MED, 9(5), 1999, pp. 703-708
Citations number
23
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
5
Year of publication
1999
Pages
703 - 708
Database
ISI
SICI code
0960-894X(19990308)9:5<703:PIOPFH>2.0.ZU;2-J
Abstract
Synthesis and biological evaluation of heteroarenes as reduced cysteine rep lacements are described. Of the heteroaryl groups examined with respect to FT inhibitor FTI-276 (1), pyridyl was the replacement found to be most effe ctive. Substitutions at C4 of the pyridyl moiety did not affect the in vitr o activity. Compound 9a was found to have moderate in vivo bioavailability. (C) 1999 Elsevier Science Ltd. All rights reserved.