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Issue 11, 2005
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Chemistry and biology of wortmannin

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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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The article was received on 30 Mar 2005, accepted on 11 Apr 2005 and first published on 20 Apr 2005

Article type: Perspective
DOI: 10.1039/B504418A
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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