Rh(III)‐Catalyzed Redox‐Neutral [4+2] Annulation for Direct Assembly of 3‐Acyl Isoquinolin‐1(2H)‐ones as Potent Antitumor Agents

Abstract By virtue of an efficient rhodium(III)‐catalyzed redox‐neutral C−H activation/ring‐opening of a strained ring/[4+2] annulation cascade of N ‐methoxybenzamides with propargyl cycloalkanols, diverse 3‐acyl isoquinolin‐1(2 H )‐ones were directly obtained in good yields and with excellent functional group compatibility. Additionally, their antitumor activities against various human cancer cells including HepG2, A549, MCF‐7 and SH‐SY5Y were evaluated and the action mechanism of the selected compound was also investigated in vitro . The results revealed that these products possessed a potent efficacy, by inhibiting proliferation and inducing apoptosis in a time‐dependent and dose‐dependent manner, suggesting that such compounds can serve as promising candidates for anti lung cancer drug discovery.