The squalestatins: potent inhibitors of squalene synthase. The role of the tricarboxylic acid moiety

Watson, Nigel S, Bell, Richard, Chan, Chuen, Cox, Brian, Hutson, Julie L, Keeling, Suzanne E, Kirk, Barrie E, Procopiou, Panayiotis A, Steeples, Ian P and Widdowson, Julia (1993) The squalestatins: potent inhibitors of squalene synthase. The role of the tricarboxylic acid moiety. Bioorganic and Medicinal Chemistry Letters, 3 (12). pp. 2541-2546. ISSN 0960-894X

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Abstract

In squalestatins possessing at C6 either a 4,6-dimethyloctenoate ester or a hydroxyl group, the 5-carboxylic acid is crucial for squalene synthase inhibitory activity. In the former seires, free carboxylic acids are not required at C3 or C4 for potent enzyme inhibitory activity whereas in the latter series esterification of the carboxylic acids at C3 or C4 results in a significant reduction in enzyme inhibitory activity.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Subjects: Q Science > QD Chemistry
Depositing User: Tom Gittoes
Date Deposited: 14 Jan 2015 10:10
Last Modified: 14 Jan 2015 10:10
URI: http://sro.sussex.ac.uk/id/eprint/52124
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