1083236-25-2

Upstream product

• 95-54-5 1,2-diamino-benzene 
• 15804-19-0 quinoxaline-2,3-dione 
• 2213-63-0 2,3-dichloroquinoxaline 
• 2297-64-5 p-bromophenylsulfonyl hydrazide 

Downstream Products

• 1203551-17-0 2-(4-chlorophenylamino)-3-(4-bromophenylsulfonyl)quinoxaline 
• 1345670-31-6 2-(3-hydroxyphenylamino)-3-(4-bromophenylsulfonyl)quinoxaline 
• 1345670-32-7 2-(4-fluorophenylamino)-3-(4-bromophenylsulfonyl)quinoxaline 
• 1203551-43-2 2-(3,4-dihydroisoquinolin-2(1H)-yl)-3-(4-bromophenylsulfonyl)quinoxaline 
• 1350960-66-5 2-(4-hydroxypiperidin-1-yl)-3-(4-bromophenylsulfonyl)quinoxaline 
• 1350960-70-1 2-(3-hydroxypiperidin-1-yl)-3-(4-bromophenylsulfonyl)quinoxaline 
• 1203551-42-1 2-(pyrrolidin-1-yl)-3-(4-bromophenylsulfonyl)quinoxaline 

Relevant academic research and scientific papers

Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl) quinoxalines as PI3Kα inhibitors

A series of novel 2-arylamino-3-(arylsulfonyl)quinoxalines was synthesized through a newly developed approach. All synthesized target compounds were screened for their cytotoxicities against cancer cell lines including PC3, A549, HCT116, HL60 and KB. Representative compounds with favorable cytotoxicities were tested for their PI3Kα inhibitory activities. Among the synthesized target compounds, 17 (PI3Kα IC50: 0.07 μM) displayed the most potent cellular activities (IC50 values of 0.14 μM, 0.07 μM, 0.95 μM and 0.05 μM against PC3, A549, HCT116 and HL 60, respectively).

Discovery of novel 2-piperidinol-3-(arylsulfonyl)quinoxalines as phosphoinositide 3-kinase α (PI3Kα) inhibitors

A series of novel 2-aliphatic cyclic amine-3-(arylsulfonyl)quinoxalines was synthesized based on the structural features of a previously identified lead, WR1. The 2-piperidinol-3-(arylsulfonyl)quinoxalines, which showed excellent antitumor activities against five human cell lines, with inhibitory activities ranging from 0.34 to 2.32 μM, proved to be a promising class of novel PI3Kα inhibitors. The most potent compound 10d (WR23) showed an inhibitory IC50 value of 0.025 μM against PI3Kα and significant pAkt suppression effect. Molecular docking analysis was performed to determine possible binding modes between PI3Kα and target compounds.