Antimalarial activity of 2,6-dibenzylidenecyclohexanone derivatives
[Display omitted] Malaria remains one of the deadliest infectious diseases worldwide and continues to infect hundreds of millions of individuals each year. Here we report the discovery and derivatization of a series of 2,6-dibenzylidenecyclohexanones targeting the chloroquine-sensitive 3D7 strain of...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2021-09, Vol.47, p.128216-128216, Article 128216 |
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Hauptverfasser: | , , , , , , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Online-Zugang: | Volltext |
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Zusammenfassung: | [Display omitted]
Malaria remains one of the deadliest infectious diseases worldwide and continues to infect hundreds of millions of individuals each year. Here we report the discovery and derivatization of a series of 2,6-dibenzylidenecyclohexanones targeting the chloroquine-sensitive 3D7 strain of Plasmodium falciparum . While the initial lead compound displayed significant toxicity in a human cell proliferation assay, we were able to identify a derivative with no detectable toxicity and sub-micromolar potency. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2021.128216 |