The discovery, synthesis and antimalarial evaluation of natural product-based polyamine alkaloids
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Author(s)
Choomuenwai, Vanida
Schwartz, Brett D
Beattie, Karren D
Andrews, Katherine T
Khokhar, Shahan
Davis, Rohan A
Year published
2013
Metadata
Show full item recordAbstract
Bioassay-guided fractionation of an antimalarial extract derived from the fungus Ramaria subaurantiaca afforded the known polyamine alkaloid, pistillarin. Nine pistillarin analogues were synthesised via EDC-mediated chemistry and these compounds along with the previously reported natural product polyamines, ianthelliformisamines A-C and spermatinamine, were evaluated against Plasmodium falciparum (3D7) parasites and a normal human cell line to determine parasite-specific activity. Spermatinamine (IC50 0.23 卩 and pistillarin (IC50 1.9 卩 were the two most potent antimalarials identified during these studies.Bioassay-guided fractionation of an antimalarial extract derived from the fungus Ramaria subaurantiaca afforded the known polyamine alkaloid, pistillarin. Nine pistillarin analogues were synthesised via EDC-mediated chemistry and these compounds along with the previously reported natural product polyamines, ianthelliformisamines A-C and spermatinamine, were evaluated against Plasmodium falciparum (3D7) parasites and a normal human cell line to determine parasite-specific activity. Spermatinamine (IC50 0.23 卩 and pistillarin (IC50 1.9 卩 were the two most potent antimalarials identified during these studies.
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Journal Title
Tetrahedron Letters
Volume
54
Copyright Statement
© 2013 Elsevier. This is the author-manuscript version of this paper. Reproduced in accordance with the copyright policy of the publisher. Please refer to the journal's website for access to the definitive, published version.
Subject
Medicinal and biomolecular chemistry
Biologically active molecules
Organic chemistry
Medical parasitology
Biochemistry and cell biology