1312448-27-3

Upstream product

• 1112982-79-2 N-(5-bromo-2-chloro-3-pyridinyl)-4-fluoro-N-((4-fluorophenyl)sulfonyl)benzenesulfonamide 
• 349-88-2 4-Fluorobenzenesulfonyl chloride 
• 887309-87-7 N-(5-bromo-2-chloro-pyridine-3-yl)-4-fluorobenzenesulfonamide 
• 588729-99-1 3-amino-5-bromo-2-chloropyridine 
• 53218-26-1 6-bromo-1,3-benzothiazole 
• 1112983-31-9 N-(2-chloro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-3-yl)-4-fluorobenzenesulfonamide 

Relevant academic research and scientific papers

Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: Discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives

The phosphoinositide 3-kinase (PI3K) family catalyzes the ATP-dependent phosphorylation of the 3′-hydroxyl group of phosphatidylinositols and plays an important role in cell growth and survival. There is abundant evidence demonstrating that PI3K signaling is dysregulated in many human cancers, suggesting that therapeutics targeting the PI3K pathway may have utility for the treatment of cancer. Our efforts to identify potent, efficacious, and orally available PI3K/mammalian target of rapamycin (mTOR) dual inhibitors resulted in the discovery of a series of substituted quinolines and quinoxalines derivatives. In this report, we describe the structure-activity relationships, selectivity, and pharmacokinetic data of this series and illustrate the in vivo pharmacodynamic and efficacy data for a representative compound.

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

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