OREGANIC ACID - A POTENT NOVEL INHIBITOR OF RAS FARNESYL-PROTEIN TRANSFERASE FROM AN ENDOPHYTIC FUNGUS

Authors
JAYASURIYA H BILLS GF CASCALES C ZINK DL GOETZ MA JENKINS RG SILVERMAN KC LINGHAM RB SINGH SB
Citation
H. Jayasuriya et al., OREGANIC ACID - A POTENT NOVEL INHIBITOR OF RAS FARNESYL-PROTEIN TRANSFERASE FROM AN ENDOPHYTIC FUNGUS, Bioorganic & medicinal chemistry letters, 6(17), 1996, pp. 2081-2084
Citations number
20
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
17
Year of publication
1996
Pages
2081 - 2084
Database
ISI
SICI code
0960-894X(1996)6:17<2081:OA-APN>2.0.ZU;2-Q
Abstract
Inhibitors of farnesyl-protein transferase (FPTase) have the potential of being anticancer agents for tumors in which ras is found mutated a nd contributes to cell transformation. From the screening of the extra cts tricarboxylated alkylsulfate, oreganic acid (1), as a potent (IC50 = 14 nM) and specific inhibitor of FPTase. Its desulfated analog (4) was less active (IC50 = 3.3 mu M). The trimethylester (2) and its desu lfated analog (3) were inactive. Copyright (C) 1996 Elsevier Science L td