期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 51, 期 18, 页码 5522-5532出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm800295d
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资金
- U.S. Department of Energy [DE-AC03-76SF00098]
- Lawrence Berkeley National Laboratory
- The Institute of Cancer Research
- Cancer Research UK [C309/A8724, C2536/A5708]
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 pl 110 alpha. 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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