Synthesis and activity of β-carboline antimalarials targeting the Plasmodium falciparum heat shock 90 protein

[Display omitted] A collection of β-carbolines based on the natural product harmine, a compound known to target the heat shock 90 protein of Plasmodium falciparum, was synthesized and tested for antimalarial activity and potential toxicity. Several of these novel compounds display promising bioactiv...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2023-08, Vol.92, p.129410, Article 129410
Main Authors: Viswanathan, Neil K., Chirgwin, Michael E., Gibbs, Julia, Kalaj, Brianna N., Durham, Sierra, Tran, Jennifer, Gomez, Maximillian, Lazaro, Horacio, Chen, Ming, Mansfield, Christopher R., Derbyshire, Emily R., Eagon, Scott
Format: Article
Language:English
Subjects:
Antimalarials - pharmacology
Beta-carbolines
Carbolines - pharmacology
Heat shock 90 protein
Heat-Shock Response
HSP90 Heat-Shock Proteins - antagonists & inhibitors
Malaria
Plasmodium falciparum
Protozoan Proteins - antagonists & inhibitors
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Summary:[Display omitted] A collection of β-carbolines based on the natural product harmine, a compound known to target the heat shock 90 protein of Plasmodium falciparum, was synthesized and tested for antimalarial activity and potential toxicity. Several of these novel compounds display promising bioactivity, providing a new potential therapeutic with a mode of action that differs versus any currently available clinical treatment.
ISSN:0960-894X
1464-3405
1464-3405
DOI:10.1016/j.bmcl.2023.129410