The DOI matches its Crossref record; 5 of the 5 references it cites were found in a registry or an index.
The Identification of 2-(1 H-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
Open accessAbstract
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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Cites
The phosphoinositide 3-kinase pathway
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Mutant PIK3CA promotes cell growth and invasion of human cancer cells.
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Targeting PI3K/Akt signal transduction for cancer therapy
He, Y., Sun, M. M., Zhang, G. G., Yang, J., Chen, K. S., Xu, W. W., & Li, B. (2021) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-021-00828-5 · Cited by 1,892
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Proteogenomic characterization of pancreatic ductal adenocarcinoma
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Frequent Activating Mutations of PIK3CA in Ovarian Clear Cell Carcinoma
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Metadata
- Authors
- 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. A., Wan, N. C., Wiesmann, C., Workman, P., Zhyvoloup, A., Zvelebil, M. J., & Shuttleworth, S. J.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2008-08-29
- Volume
- 51
- Issue
- 18
- Pages
- 5522-5532
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2029754521
- Cited by
- 741
- References
- 5
- FWCI
- 17.25
- Type
- journal article
- Language
- en
- Open access
- green
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