Naphthylisoquinoline alkaloids, validated as hit multistage antiplasmodial natural products.

ABSTRACT: The discovery and development of multistage antimalarial drugs targeting intra-erythrocytic asexual and sexual Plasmodium falciparum parasites is of utmost importance to achieve the ambitious goal of malaria elimination. Here, we report the validation of naphthylisoquinoline (NIQ) alkaloids and their synthetic analogues as multistage active antimalarial drug candidates. A total of 30 compounds were tested, of which 17 exhibited IC₅₀ values <1 μM against drug-sensitive P. falciparum parasites (NF54 strain); 15 of these retained activity against a panel of drug-resistant strains. These compounds showed low in vitro cytotoxicity against HepG2 cells, with selectivity indices of >10. The tested compounds showed activity in vitro against both early- and late-stage P. falciparum gameto

SUBMITTER: Moyo P 

PROVIDER: S-EPMC7270141 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature