7-Chloroquinolinotriazoles: Synthesis by the azide–alkyne cycloaddition click chemistry, antimalarial activity, cytotoxicity and SAR studies

…, GC Brandão, LM Arantes, HA de Oliveira…

Index: Pereira, Guilherme R.; Brandao, Geraldo Celio; Arantes, Lucas M.; De Oliveira Jr., Haliton A.; De Paula, Renata Cristina; Do Nascimento, Maria Fernanda A.; Dos Santos, Fabio M.; Da Rocha, Ramon K.; Lopes, Julio Cesar D.; De Oliveira, Alaide Braga European Journal of Medicinal Chemistry, 2014 , vol. 73, p. 295 - 309

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Citation Number: 16

Abstract

Abstract Twenty-seven 7-chloroquinolinotriazole derivatives with different substituents in the triazole moiety were synthesized via copper-catalyzed cycloaddition (CuAAC) click chemistry between 4-azido-7-chloroquinoline and several alkynes. All the synthetic compounds were evaluated for their in vitro activity against Plasmodium falciparum (W2) and cytotoxicity to Hep G2A16 cells. All the products disclosed low cytotoxicity (CC 50> ...