Synthesis and activity of β-carboline antimalarials targeting the Plasmodium falciparum heat shock 90 protein.
Publication
, Journal Article
Viswanathan, NK; Chirgwin, ME; Gibbs, J; Kalaj, BN; Durham, S; Tran, J; Gomez, M; Lazaro, H; Chen, M; Mansfield, CR; Derbyshire, ER; Eagon, S
Published in: Bioorganic & medicinal chemistry letters
August 2023
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.
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Published In
Bioorganic & medicinal chemistry letters
DOI
EISSN
1464-3405
ISSN
0960-894X
Publication Date
August 2023
Volume
92
Start / End Page
129410
Related Subject Headings
- Protozoan Proteins
- Plasmodium falciparum
- Medicinal & Biomolecular Chemistry
- Heat-Shock Response
- HSP90 Heat-Shock Proteins
- Carbolines
- Antimalarials
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry
- 1115 Pharmacology and Pharmaceutical Sciences
Citation
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Chicago
ICMJE
MLA
NLM
Viswanathan, N. K., Chirgwin, M. E., Gibbs, J., Kalaj, B. N., Durham, S., Tran, J., … Eagon, S. (2023). Synthesis and activity of β-carboline antimalarials targeting the Plasmodium falciparum heat shock 90 protein. Bioorganic & Medicinal Chemistry Letters, 92, 129410. https://doi.org/10.1016/j.bmcl.2023.129410
Viswanathan, Neil K., Michael E. Chirgwin, Julia Gibbs, Brianna N. Kalaj, Sierra Durham, Jennifer Tran, Maximillian Gomez, et al. “Synthesis and activity of β-carboline antimalarials targeting the Plasmodium falciparum heat shock 90 protein.” Bioorganic & Medicinal Chemistry Letters 92 (August 2023): 129410. https://doi.org/10.1016/j.bmcl.2023.129410.
Viswanathan NK, Chirgwin ME, Gibbs J, Kalaj BN, Durham S, Tran J, et al. Synthesis and activity of β-carboline antimalarials targeting the Plasmodium falciparum heat shock 90 protein. Bioorganic & medicinal chemistry letters. 2023 Aug;92:129410.
Viswanathan, Neil K., et al. “Synthesis and activity of β-carboline antimalarials targeting the Plasmodium falciparum heat shock 90 protein.” Bioorganic & Medicinal Chemistry Letters, vol. 92, Aug. 2023, p. 129410. Epmc, doi:10.1016/j.bmcl.2023.129410.
Viswanathan NK, Chirgwin ME, Gibbs J, Kalaj BN, Durham S, Tran J, Gomez M, Lazaro H, Chen M, Mansfield CR, Derbyshire ER, Eagon S. Synthesis and activity of β-carboline antimalarials targeting the Plasmodium falciparum heat shock 90 protein. Bioorganic & medicinal chemistry letters. 2023 Aug;92:129410.
Published In
Bioorganic & medicinal chemistry letters
DOI
EISSN
1464-3405
ISSN
0960-894X
Publication Date
August 2023
Volume
92
Start / End Page
129410
Related Subject Headings
- Protozoan Proteins
- Plasmodium falciparum
- Medicinal & Biomolecular Chemistry
- Heat-Shock Response
- HSP90 Heat-Shock Proteins
- Carbolines
- Antimalarials
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry
- 1115 Pharmacology and Pharmaceutical Sciences