The squalestatins: Potent inhibitors of squalene synthase, 3-hydroxymethyl derivatives

A series of 3-hydroxymethyl derivatives of squalestatin 1 was prepared as inhibitors of squalene synthase. Potent in vitro inhibitory activity is retained in those analogues which possess C-6 and C-1 substituents analogous to those found in 1. A series of 3-hydroxymethyl derivatives of squalestatin...

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Published inBioorganic & medicinal chemistry letters Vol. 4; no. 16; pp. 1931 - 1936
Main Authors Cox, Brian, Hutson, Julie L., Keeling, Suzanne E., Kirk, Barrie E., Srikantha, Anton R.P., Watson, Nigel S.
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 25.08.1994
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Summary:A series of 3-hydroxymethyl derivatives of squalestatin 1 was prepared as inhibitors of squalene synthase. Potent in vitro inhibitory activity is retained in those analogues which possess C-6 and C-1 substituents analogous to those found in 1. A series of 3-hydroxymethyl derivatives of squalestatin 1 was prepared as inhibitors of squalene synthase. Potent in vitro inhibitory activity is retained in 5 and in those analogues which possess C-6 and C-1 substituents closely similar to those found in 1.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)80537-0