Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 30, Issue 21, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127502
Keywords
Malaria; Plasmodium falciparum; Tetrahydro-beta-carbolines; Structure activity relationship; Structure based design
Categories
Funding
- Center for Applied Biotechnology at California Polytechnic State University
- Bill and Linda Frost Fund
- Grand Challenges Canada
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A series of tetrahydro-beta-carboline derivatives of a lead compound known to target the heat shock 90 protein of Plasmodium falciparum were synthesized and assayed for both potency against the parasite and toxicity against a human cell line. Using a rationalized structure based design strategy, a new lead compound with a potency two orders of magnitude greater than the original lead compound was found. Additional modeling of this new lead compound suggests multiple avenues to further increase potency against this target, potentially paving the path for a therapeutic with a mode of action different than any current clinical treatment.
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