Palladium-catalyzed domino sequence for the synthesis of N-aryl quinolinone-3-carboxylate derivatives and their anti-proliferative activity |
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| Authors: | NS Kameswara Rao Korupolu Raghu Babu |
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| Institution: | 1. GVK Biosciences Private Limited, Medicinal Chemistry Laboratory, Hyderabad 500076, India;2. Andhra University, Department of Engineering Chemistry, Andhra University College of Engineering (A), Visakhapatnam 530003, India |
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| 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 0.41 µM to 45.77 µM. Among them, compounds 6j, 6k and 6m demonstrated potential activity particularly against MCF-7 (breast) and KB (oral) cancer cell lines. |
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| Keywords: | Domino reaction Buchwald coupling Cyclization Cytotoxicity |
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