Abstract

UMUMARARUNGU, Théoneste et al. Re-screening and preliminary in vitro evaluation of resorcinol based Hsp90 inhibitors for potential protocidal activity. S.Afr.j.chem. (Online) [online]. 2023, vol.77, pp.24-29. ISSN 1996-840X.  http://dx.doi.org/10.17159/0379-4350/2023/v77a04.

This study explored a series of resorcinol derivatives originally identified as heat shock protein 90 inhibitors for activity against protozoan parasites. The repurposing of this series revealed that some of these compounds are active against chloroquine-sensitive Plasmodium falciparum (3D7) and Trypanosoma brucei brucei strains with IC₅₀ values below 10 μM without obvious cytotoxic effects against human cervix adenocarcinoma (HeLa) cells at 25 μM.

Keywords : drug-likeness; Plasmodium falciparum; resorcinol derivatives; sleeping sickness; Trypanosoma brucei brucei.

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