NOVEL TRICYCLIC AMINOACETYL AND SULFONAMIDE INHIBITORS OF RAS FARNESYL-PROTEIN TRANSFERASE

Authors
NJOROGE FG VIBULBHAN B ALVAREZ CS BISHOP WR PETRIN J DOLL RJ GIRIJAVALLABHAN V GANGULY AK
Citation
Fg. Njoroge et al., NOVEL TRICYCLIC AMINOACETYL AND SULFONAMIDE INHIBITORS OF RAS FARNESYL-PROTEIN TRANSFERASE, Bioorganic & medicinal chemistry letters, 6(24), 1996, pp. 2977-2982
Citations number
30
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
24
Year of publication
1996
Pages
2977 - 2982
Database
ISI
SICI code
0960-894X(1996)6:24<2977:NTAASI>2.0.ZU;2-4
Abstract
Novel tricyclic FPT inhibitors with submicromolar FPT activity are des cribed. Greatly enhanced FPT activity is realized with phthaloyl deriv atized amino compound 2k, which showed FPT inhibitory activity of IC50 = 0.66 mu M. Sulfonamides 5g and 50 were also found to be potent FPT inhibitor. SAR resulting from a variety of tricyclic amino acids and s ulfonamide derivatives is discussed. Copyright (C) 1996 Elsevier Scien ce Ltd