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

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

  • Bioorg Med Chem Lett. 2023 Aug 15;92:129410. doi: 10.1016/j.bmcl.2023.129410.
Neil K Viswanathan 1,  Michael E Chirgwin 2,  Julia Gibbs 1,  Brianna N Kalaj 3,  Sierra Durham 4,  Jennifer Tran 1,  Maximillian Gomez 1,  Horacio Lazaro 5,  Ming Chen 5,  Christopher R Mansfield 6,  Emily R Derbyshire 2,  Scott Eagon 7
Affiliations

Affiliations

  • 1 Department of Chemistry & Biochemistry, California Polytechnic State University, San Luis Obispo, CA 93407, USA.
  • 2 Department of Chemistry, Duke University, Durham, NC 27708, USA.
  • 3 Department of Chemistry and Biochemistry, University of California, San Diego, La Jolla, CA 92093, USA.
  • 4 Department of Food Science and Technology, University of California, Davis, Davis, CA 95616, USA.
  • 5 Promega Biosciences, 277 Granada Drive, San Luis Obispo, CA 93401, USA.
  • 6 Department of Molecular Genetics and Microbiology, Duke School of Medicine, Durham, NC 27708, USA.
  • 7 Department of Chemistry & Biochemistry, California Polytechnic State University, San Luis Obispo, CA 93407, USA. Electronic address: [email protected].
PMID: 37478957 DOI: 10.1016/j.bmcl.2023.129410
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.

Keywords

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

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