1. Synthesis and activity of β-carboline antimalarials targeting the Plasmodium falciparum heat shock 90 protein.
- Author
-
Viswanathan NK, Chirgwin ME, Gibbs J, Kalaj BN, Durham S, Tran J, Gomez M, Lazaro H, Chen M, Mansfield CR, Derbyshire ER, and Eagon S
- Subjects
- Carbolines pharmacology, Heat-Shock Response, Plasmodium falciparum, Antimalarials pharmacology, Protozoan Proteins antagonists & inhibitors, HSP90 Heat-Shock Proteins antagonists & inhibitors
- Abstract
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., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 The Authors. Published by Elsevier Ltd.. All rights reserved.)
- Published
- 2023
- Full Text
- View/download PDF