The antiplasmodial activity of norcantharidin analogs

Title: The antiplasmodial activity of norcantharidin analogs
Creator: Bajsa, Joanna; McCluskey, Adam; Gordon, Christopher P.; Stewart, Scott G.; Hill, Timothy A.; Sahu, Rajnish; Duke, Stephen O.; Tekwani, Babu L.
Relation: Bioorganic & Medicinal Chemistry Letters Vol. 20, Issue 22, p. 6688-6695
Publisher Link: http://dx.doi.org/10.1016/j.bmcl.2010.09.004
Publisher: Elsevier
Resource Type: journal article
Date: 2010
Description: The antiplasmodial activities of sixty norcantharidin analogs were tested in vitro against a chloroquine sensitive (D6, Sierra Leone) and chloroquine resistant (W2) strains of Plasmodium falciparum. Forty analogs returned IC₅₀ values <500 μM against at least one of the P. falciparum strains examined. The ring open compound 24 ((1S,4R)-3-(allylcarbamoyl)-7-oxabicyclo[2.2.1]heptane-2-carboxylic acid) is the most active aliphatic analog (D6 IC₅₀ = 3.0 ± 0.0 and W2 IC₅₀ = 3.0 ± 0.8 μM) with a 20-fold enhancement relative to norcantharidin. Surprisingly, seven norcantharimides also displayed good antiplasmodial activity with the most potent, 5 returning D6 = 8.9 ± 0.9 and W2 IC₅₀ = 12.5 ± 2.2 μM, representing a fivefold enhancement over norcantharidin.
Subject: Plasmodium falciparum; antimalarial drugs; cantharidin; protein phosphatase inhibitors
Identifier: http://hdl.handle.net/1959.13/921629
Identifier: uon:9348
Identifier: ISSN:0960-894X
Language: eng
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