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Bioorg Med Chem. 2011 Nov 15;19(22):6615-9. doi: 10.1016/j.bmc.2011.06.006. Epub 2011 Jun 12.

Convolutamines I and J, antitrypanosomal alkaloids from the bryozoan Amathia tortusa.

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1
Eskitis Institute, Griffith University, Brisbane, QLD 4111, Australia.

Abstract

Mass-directed isolation of the CH(2)Cl(2)/CH(3)OH extract from the marine bryozoan Amathia tortusa resulted in the purification of two new brominated alkaloids, convolutamines I (1) and J (2). The structures of 1 and 2 were determined following spectroscopic data analysis. Both compounds were isolated during a drug discovery program aimed at identifying new antitrypanosomal leads from a prefractionated natural product library. Compounds 1 and 2 were shown to be active toward the parasite Trypanosoma brucei brucei with IC(50) values of 1.1 and 13.7 μM, respectively. Preliminary toxicity profiling was also performed on both 1 and 2 using the human embryonic kidney cell line, HEK293. Compound 1 was shown to exhibit cytotoxicity against HEK293 with an IC(50) of 22.0 μM whilst 2 was inactive at 41.0 μM.

PMID:
21705225
DOI:
10.1016/j.bmc.2011.06.006
[Indexed for MEDLINE]

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