1162680-35-4Relevant articles and documents
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.
, 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