Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 19, Issue 22, Pages 6604-6607Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.05.046
Keywords
Fascaplysin analogues; Ascidian; Antimalarial; Absolute configuration; Experimental and theoretically calculated ECD
Funding
- NIH [RR06262, CA36622]
- International Society for Advancement of Cytometry Scholars Program
- CWRU
- USDA Agricultural Research Service [58-6408-2-0009]
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A new fascaplysin analogue, 3-bromohomofascaplysin A (1), along with two known analogues, homofascaplysin A (2) and fascaplysin (3), were isolated from a Fijian Didemnum sp. ascidian. The absolute configurations of 3-bromohomofascaplysin A (1) and homofascaplysin A (2) were determined via experimental and theoretically calculated ECD spectra. The differential activities of 1-3 against different blood-borne life stages of the malaria pathogen Plasmodium falciparum were assessed. Homofascaplysin A (2) displayed an IC(50) of 0.55 +/- 0.11 nM against ring stage parasites and 105 +/- 38 nM against all live parasites. Given the stronger resistance of ring stage parasites against most current antimalarials relative to the other blood stages, homofascaplysin A (2) represents a promising agent for treatment of drug resistant malaria. (C) 2011 Elsevier Ltd. All rights reserved.
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