Palladium-catalyzed domino sequence for the synthesis of N-aryl quinolinone-3-carboxylate derivatives and their anti-proliferative activity

Abstract

An efficient and an operationally simple Palladium-catalyzed domino reaction for the synthesis of N-aryl quinolinone-3-carboxylate derivatives has been developed via the reaction between diethyl 2-(2-bromobenzylidine) malonate and anilines. These newly synthesized compounds exhibited good to moderate anti-proliferative activity with GI50 values ranging from 0.41µM to 45.77µM. Among them, compounds 6j, 6k and 6m demonstrated potential activity particularly against MCF-7 (breast) and KB (oral) cancer cell lines.