Synthesis and antiproliferative activities of OSW-1 analogues bearing 2-acylamino-xylose residues. Issue 14 (23rd May 2019)

• Record Type: Journal Article
• Authors: Sun, Lijun; Wang, Ruina; Wang, Xiaobo; Dang, Yongjun; Li, Wei; Yu, Biao
• Is Part Of: Organic chemistry frontiers. Volume 6:Issue 14(2019)
• Page Start: 2385
• Page End: 2391
• Publication Date: 2019-05-23
• Subjects: Chemistry, Organic -- Periodicals; 547.005
• DOI: 10.1039/c9qo00462a
• Languages: English
• ISSNs: 2052-4110

Abstract

Abstract : We synthesized 38 OSW-1 analogues with 2-acylamino xylose residues and found that the antitumor activities could be greatly enhanced. 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.