THE SQUALESTATINS - POTENT INHIBITORS OF SQUALENE SYNTHASE - THE ROLEOF THE TRICARBOXYLIC-ACID MOIETY

Authors
WATSON NS BELL R CHAN C COX B HUTSON JL KEELING SE KIRK BE PROCOPIOU PA STEEPLES IP WIDDOWSON J
Citation
Ns. Watson et al., THE SQUALESTATINS - POTENT INHIBITORS OF SQUALENE SYNTHASE - THE ROLEOF THE TRICARBOXYLIC-ACID MOIETY, Bioorganic & medicinal chemistry letters, 3(12), 1993, pp. 2541-2546
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
12
Year of publication
1993
Pages
2541 - 2546
Database
ISI
SICI code
0960-894X(1993)3:12<2541:TS-PIO>2.0.ZU;2-S
Abstract
In squalestatins possessing at C6 either a 4,6-dimethyloctenoate ester or a hydroxyl group, the 5-carboxylic acid is crucial for squalene sy nthase inhibitory activity. In the former series, free carboxylic acid s are not required at C3 or C4 for potent enzyme inhibitory activity w hereas in the latter series esterification of the carboxylic acids at C3 or C4 results in a significant reduction in enzyme inhibitory activ ity.