Abstract
Zaragozic acids (or squalestatins) are very potent inhibitors of squalene synthase. They or simpler analogs have potential as drugs for lowering the endogenous level of cholesterol in human serum. These compounds are Ras farnesyltransferase inhibitors and might become antitumor drugs. They are also antifungal agents. This account presents synthetic studies subsequent to those reviewed by Nadin and Nicolaou (1). A wealth of new chemistry has been developed for the generation of highly oxygenated 2,8-dioxabicyclo(3.2.1)octane-3,4,5-tricarboxylic triacids and analogs, so demonstrating the fascination of synthetic chemists for zaragozic acids.
Keywords: Zaragozic Acids, farnesyltransferase, 3,4,5-tricarboxylic, isopentyladenine,, sterol 27-hydroxylase,, intramolecular acetalization, 5-phenylthiofuran-2-carboxylic acid, allylmagnesium bromide, 6,7-dideoxysqualestatin, Ozonolysis
Call for Papers in Thematic Issues
Catalytic C-H bond activation as a tool for functionalization of heterocycles
The major topic is the functionalization of heterocycles through catalyzed C-H bond activation. The strategies based on C-H activation not only provide straightforward formation of C-C or C-X bonds but, more importantly, allow for the avoidance of pre-functionalization of one or two of the cross-coupling partners. The beneficial impact of ...read more
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