Antimalarial activity of 2,6-dibenzylidenecyclohexanone derivatives

Scott Eagon, Jared T. Hammill, Kasey Fitzsimmons, Natalie Sienko, Brandon Nguyen, Jarvis Law, Aashrita Manjunath, Steven P. Wilkinson, Kara Thompson, Julia Elizabeth Glidden, Amy L. Rice, Mofolusho O. Falade, Joshua J. Kimball, Celine DiBernardo, R. Kiplin Guy

Research output: Contribution to journalArticlepeer-review

1 Scopus citations

Abstract

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.

Original languageEnglish
Article number128216
JournalBioorganic and Medicinal Chemistry Letters
Volume47
DOIs
StatePublished - Sep 1 2021

Bibliographical note

Funding Information:
This work was supported by the Bill and Linda Frost Fund at California Polytechnic State University (no associated grant number).

Publisher Copyright:
© 2021 The Author(s)

Keywords

  • 2,6-Dibenzylidenecyclohexanone
  • Malaria
  • Michael system
  • Plasmodium falciparum
  • Structure activity relationship

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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