The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer.

Folkes, A.J., Ahmadi, K., Alderton, W.K., Alix, S., Baker, S.J., Box, G., Chuckowree, I.S., Clarke, P.A., Depledge, P., Eccles, S.A., Friedman, L.S., Hayes, A., Hancox, T.C., Kugendradas, A., Lensun, L., Moore, P., Olivero, A.G., Pang, J., Patel, S., Pergl-Wilson, G.H., Raynaud, F.I., Robson, A., Saghir, N., Salphati, L., Sohal, S., Ultsch, M.H., Valenti, M., Wallweber, H.J., Wan, N.C., Wiesmann, C., Workman, P., Zhyvoloup, A., Zvelebil, M.J., Shuttleworth, S.J.
Journal   J Med Chem.
Species  
Analytes Measured   Akt
Matrix Tested   MDA-MB-361 and PC3 cell lysates
Year   2008
Volume   51
Page Numbers   5522-32
Application   Phosphoproteins
Abstract
Phosphatidylinositol-3-kinase (PI3K) is an important target in cancer due to the deregulation of the PI3K/ Akt signaling pathway in a wide variety of tumors. A series of thieno[3,2-d]pyrimidine derivatives were prepared and evaluated as inhibitors of PI3 kinase p110alpha. The synthesis, biological activity, and further profiling of these compounds are described. This work resulted in the discovery of 17, GDC-0941, which is a potent, selective, orally bioavailable inhibitor of PI3K and is currently being evaluated in human clinical trials for the treatment of cancer.

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