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Synthesis and antiproliferative activities of OSW-1 analogues bearing 2-acylamino-xylose residues

Abstract

OSW-1 and SBF-1 are well studied saponins with exceptionally potent anti-tumor activities. Herein, we report the syntheses of a library of 38 C22-ester analogues which imbed 2-acylamino xylose residues. SAR studies show that the introduction of the 2-acylamino xylose residues could further increase the anti-tumor activities as many as 40 folds than those of SBF-1 and the (1→3)-disaccharide linkage is crucial to the activities. A highly potent probe (3) bearing photoactivatable and clickable residues has been identified.

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Publication details

The article was received on 02 Apr 2019, accepted on 29 Apr 2019 and first published on 30 Apr 2019


Article type: Research Article
DOI: 10.1039/C9QO00462A
Org. Chem. Front., 2019, Accepted Manuscript

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    Synthesis and antiproliferative activities of OSW-1 analogues bearing 2-acylamino-xylose residues

    L. Sun, R. Wang, X. Wang, Y. Dang, W. Li and B. Yu, Org. Chem. Front., 2019, Accepted Manuscript , DOI: 10.1039/C9QO00462A

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