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Antiproliferative Activity of Amathaspiramide Alkaloids and Analogs
Jun Shimokawa1, Koji Chiyoda, Hirotatsu Umihara
1Graduate School of Pharmaceutical Sciences, Nagoya University.
Abstract:
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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