1112982-47-4Relevant academic research and scientific papers
Structure-activity relationships of phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: Investigations of various 6,5-heterocycles to improve metabolic stability
Stec, Markian M.,Andrews, Kristin L.,Booker, Shon K.,Caenepeel, Sean,Freeman, Daniel J.,Jiang, Jian,Liao, Hongyu,McCarter, John,Mullady, Erin L.,San Miguel, Tisha,Subramanian, Raju,Tamayo, Nuria,Wang, Ling,Yang, Kevin,Zalameda, Leeanne P.,Zhang, Nancy,Hughes, Paul E.,Norman, Mark H.
experimental part, p. 5174 - 5184 (2011/09/16)
N-(6-(6-Chloro-5-(4-fluorophenylsulfonamido)pyridin-3-yl)benzo[d] thiazol-2-yl)acetamide (1) is a potent and efficacious inhibitor of PI3Kα and mTOR in vitro and in vivo. However, in hepatocyte and in vivo metabolism studies, 1 was found to undergo deacet
PI3 KINASE MODULATORS AND METHODS OF USE
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Page/Page column 143, (2009/03/07)
The present invention comprises a new class of compounds capable of modulating the activity of PI3 kinase and, accordingly, useful for treatment of PI3 kinase mediated diseases, including melanomas, carcinomas and other cancer-related conditions. The compounds have a general Formula I wherein each of A1, A2, A3, A4, X, R1 and R2 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of PI3 kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
