Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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Antiproliferative Activity of Amathaspiramide Alkaloids and Analogs
Jun ShimokawaKoji ChiyodaHirotatsu UmiharaTohru Fukuyama
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2016 年 64 巻 8 号 p. 1239-1241

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Assisted by the total syntheses of all the amathaspiramides, six natural products and four synthetic intermediates with partially fluctuating structures were prepared and subjected to a growth inhibition assay in four human cancer cell lines. The results showed amathaspiramides A, C, and E had moderate antiproliferative activity. Examination of the structure–activity relationship revealed the importance of the amine or imine substructure on the pyrrolidine moiety and the 8R stereochemistry on the N-acyl hemiaminal moiety for the antiproliferative activity of amathaspiramide alkaloids.

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© 2016 The Pharmaceutical Society of Japan
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