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

► Forty five novel 2-arylamino-3-(arylsulfonyl)quinoxalines were synthesized. ► Most compounds exhibited potent in vitro cytotoxicities against tested cell lines. ► Compounds were tested as PI3Kα inhibitors. ► Compound 17 (PI3Kα IC50: 0.07 μM) showed the most potent cellular activities.