Issue 11, 2005
From the journal:

Organic & Biomolecular Chemistry

Chemistry and biology of wortmannin

Peter Wipf*a  and  Robert J. Haltera  

* Corresponding authors

a Department of Chemistry, University of Pittsburgh, Pittsburgh, U. S. A.
E-mail: pwipf@pitt.edu
Fax: +1-412-624-0787
Tel: +1-412-624-8606

Abstract

Recent synthetic and biological studies of the viridin class of steroidal furans have revealed multiple opportunities for fundamental discoveries as well as advanced drug design. Wortmannin is a potent enzyme inhibitor that binds to the ATP site of important regulatory kinases such as PI-3 kinase and Polo-like kinase. The natural product shares a unique mechanism-based biological activation pathway with other viridins. Furthermore, while there have been several encouraging approaches toward the total synthesis of these compounds, there is still ample room for improvements in synthetic strategies and tactics, and the development of structurally simplified analogs that exert more specific biological effects and are devoid of toxicity issues that have thwarted the clinical development of the parent compounds.

Graphical abstract: Chemistry and biology of wortmannin

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Article information

DOI
https://doi.org/10.1039/B504418A
Article type
Perspective
Submitted
30 Mar 2005
Accepted
11 Apr 2005
First published
20 Apr 2005

Org. Biomol. Chem., 2005,3, 2053-2061

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Chemistry and biology of wortmannin

P. Wipf and R. J. Halter, Org. Biomol. Chem., 2005, 3, 2053 DOI: 10.1039/B504418A

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