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Synthetic and computational studies on liphagal: a natural product inhibitor of PI-3K

✍ Scribed by Yanzhong Zhang; E. Zachary Oblak; Erin S.D. Bolstad; Amy C. Anderson; Jerry P. Jasinski; Ray J. Butcher; Dennis L. Wright

Book ID: 104098341
Publisher: Elsevier Science
Year: 2010
Tongue: French
Weight: 485 KB
Volume: 51
Category: Article
ISSN: 0040-4039
DOI: 10.1016/j.tetlet.2010.09.058

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✦ Synopsis

The natural product liphagal has been shown to function as a reasonably potent and selective inhibitor of the key signaling enzyme PI-3Ka. We have been interested in developing an analog class of PI-3K inhibitors based upon this unusual terpenoid natural product. Toward that end, we have evaluated the binding of the natural product to its target protein computationally and formulated a class of simplified analogs based on the structural analysis. Utilizing the cycloadduct derived from tetrabromocyclopropene and furan, we were able to generate a key, versatile scaffold upon which to pursue this analog design.

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