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Exploration of benzofuran-based compounds as potent and selective Plasmodium falciparum glycogen synthase kinase-3 (PfGSK-3) inhibitors

Bioorg Chem. 2021-03; 
Chantalle Moolman, Rencia van der Sluis, Richard M Beteck, Lesetja J Legoabe
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摘要

Plasmodium falciparum glycogen synthase kinase-3 (PfGSK-3) has been identified as a potential target for the development of novel drugs against multi-drug resistant malaria. A series of benzofuran-based compounds was synthesised and evaluated as inhibitors of recombinantly expressed and purified PfGSK-3 and human glycogen synthase kinase-3 beta (HsGSK-3β). Of this series, five compounds (5k, 5m, 5p, 5r, 5s) preferentially inhibited PfGSK-3, with four of these compounds exhibiting IC values in the sub-micromolar range (0.00048-0.440 µM). Evaluation of the structure-activity relationships required for PfGSK-3 selective inhibition indicated that a C6-OCH substitution on ring A is preferred, while the effect of ... More

关键词

Benzofurans, Glycogen synthase kinase-3, Malaria, PfGSK-3, Plasmodium falciparum, Protein kinase, Structure-activity relationship