Issue 14, 2019

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 antitumor activities. Herein, we report the syntheses of a library of 38 C22-ester analogues bearing 2-acylamino xylose residues. SAR studies show that the introduction of the 2-acylamino xylose residues could further increase the antitumor 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.

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

Supplementary files

Article information

Article type
Research Article
Submitted
02 apr 2019
Accepted
29 apr 2019
First published
30 apr 2019

Org. Chem. Front., 2019,6, 2385-2391

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, 6, 2385 DOI: 10.1039/C9QO00462A

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