4.5 Article

Synthesis and activity of & beta;-carboline antimalarials targeting the Plasmodium falciparum heat shock 90 protein

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 92, Issue -, Pages -

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2023.129410

Keywords

Malaria; Plasmodium falciparum; Beta-carbolines; Heat shock 90 protein

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A series of & beta;-carbolines based on harmine were synthesized and tested for antimalarial activity and toxicity. Some of these compounds showed promising bioactivity, offering a new therapeutic option with a unique mode of action compared to current clinical treatments.
A collection of & beta;-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.

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