Synthesis and evaluation of the antiplasmodial activity of novel indeno[2,1-c]quinoline derivatives

With the aim to explore the potentiality of new chemical scaffolds for the design of new antimalarials, a set of new indeno[2,1-c]quinolines bearing different basic heads has been synthesized and tested in vitro against chloroquine sensitive (CQ-S) and chloroquine resistant (CQ-R) strains of Plasmodium falciparum. Most of the synthesized compounds exhibited a moderate antiplasmodial activity, inhibiting the growth of both CQ-S and CQ-R strains of P. falciparum with IC50 ranging from 0.24 to 6.9 mu M and with a very low resistance index. The most potent compounds (1.2-1.3-fold the CQ on the W-2 strain) can be considered as promising 'lead compounds' to be further optimized to improve efficacy and selectivity against Plasmodia. (C) 2014 Elsevier Ltd. All rights reserved.