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 …
AJ Folkes, K Ahmadi, WK Alderton, S Alix… - Journal of medicinal …, 2008 - ACS Publications
AJ Folkes, K Ahmadi, WK Alderton, S Alix, SJ Baker, G Box, IS Chuckowree, PA Clarke…
Journal of medicinal chemistry, 2008•ACS PublicationsPhosphatidylinositol-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 p110α. 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 …
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 p110α. 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 …
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 p110α. 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.
ACS Publications