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

Authors :
Viswanathan NK
Chirgwin ME
Gibbs J
Kalaj BN
Durham S
Tran J
Gomez M
Lazaro H
Chen M
Mansfield CR
Derbyshire ER
Eagon S
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2023 Aug 15; Vol. 92, pp. 129410. Date of Electronic Publication: 2023 Jul 20.
Publication Year :
2023

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.<br />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.<br /> (Copyright © 2023 The Authors. Published by Elsevier Ltd.. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
92
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
37478957
Full Text :
https://doi.org/10.1016/j.bmcl.2023.129410