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

journal contribution
posted on 2023-06-08, 19:32 authored by Nigel S Watson, Richard Bell, Chuen Chan, Brian Cox, Julie L Hutson, Suzanne E Keeling, Barrie E Kirk, Panayiotis A Procopiou, Ian P Steeples, Julia Widdowson
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.

History

Publication status

  • Published

Journal

Bioorganic and Medicinal Chemistry Letters

ISSN

0960-894X

Publisher

Elsevier

Issue

12

Volume

3

Page range

2541-2546

Department affiliated with

  • Chemistry Publications

Full text available

  • No

Peer reviewed?

  • Yes

Legacy Posted Date

2015-01-14

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