Bis-alkylamine Indolo [3, 2-b] quinolines as Hemozoin Ligands: Implications for Antimalarial Cytostatic and Cytocidal Activities

…, M Figueiras, M Machado, C Charneira…

Index: Paulo, Alexandra; Figueiras, Marta; MacHado, Marta; Charneira, Catarina; Lavrado, Joao; Santos, Sofia A.; Lopes, Dinora; Gut, Jiri; Rosenthal, Philip J.; Nogueira, Fatima; Moreira, Rui Journal of Medicinal Chemistry, 2014 , vol. 57, # 8 p. 3295 - 3313

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Citation Number: 4

Abstract

To get insight into the relevance of targeting hemozoin (Hz) crystals, two isomeric series, N5, N10-bis-alkylamine (2a–k) and N10, O11-bis-alkylamine (3a–k) indolo [3, 2-b] quinolines, were evaluated for their in vitro activity against chloroquine (CQ)-resistant and sensitive strains of Plasmodium falciparum. In general, compounds of series 3 were more active than isomers 2, with IC50/LD50 ranging from 25/233 nM (3i) to 1.3 (3a)/10.7 (3b) μM. SAR ...