Author/Authors :
Zhang، نويسنده , , Yanzhong and Oblak، نويسنده , , E. Zachary and Bolstad، نويسنده , , Erin S.D. and Anderson، نويسنده , , Amy C. and Jasinski، نويسنده , , Jerry P. and Butcher، نويسنده , , Ray J. and Wright، نويسنده , , Dennis L.، نويسنده ,
Abstract :
The natural product liphagal has been shown to function as a reasonably potent and selective inhibitor of the key signaling enzyme PI-3Kα. 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.
