Synthesis and anticancer evaluation of 3-substituted quinolin-4-ones and 2, 3-dihydroquinolin-4-ones

S Rajput, CR Gardner, TW Failes, GM Arndt…

Index: Rajput, Santosh; Gardner, Christopher R.; Failes, Timothy W.; Arndt, Greg M.; Black, David Stc.; Kumar, Naresh Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 1 p. 105 - 115

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Citation Number: 2

Abstract

Abstract A series of 3-aryl-5, 7-dimethoxyquinolin-4-ones 8 and 3-aryl-5, 7-dimethoxy-2, 3- dihydroquinolin-4-ones 13 were synthesized in good yields. Demethylation under a range of conditions afforded the corresponding 5-hydroxy and 5, 7-dihydroxy derivatives. Biological evaluation against a range of cancer cells lines showed that the quinolin-4-one scaffold was more cytotoxic than the reduced 2, 3-dihydroquinolin-4-one scaffold. The most active ...