Synthesis and Antiproliferative Activities of OSW-1 Analogues Bearing 2"-0-p-Acylaminobenzoyl Residues  

作　　者：Lijun Sun Di Zhu Laura Olde Groote Beverborg Ruina Wang Yongjun Dang Mingming Ma Wei Li Biao Yu 

机构地区：[1]Deportment of Chemistry,University of Science and Technology of Chino,96 Jinzhai Road,Hefei,Anhui 230026,China [2]State Key Laboratory of Bio-organic and Natural Products Chemistry,Center for Excellence in Molecular Synthesis,Shanghai Institute of Organic Chemistry,Chinese Academy of Sciences,345 Lingling Road,Shanghai 200032,China [3]Key Laboratory of Metabolism and Molecular Medicine,the Ministry of Education,Department of Biochemistry and Molecular Biology,School of Basic Medical Sciences,Fudan Uniersity,Shanghai 200032,China [4]Department of Medicinal Chemistry,China Pharmaceutical University,639 Lon gmian Avenue,Nanjing,Jiangsu 211198,China

出　　处：《Chinese Journal of Chemistry》2020年第10期1091-1097,共7页中国化学（英文版）

基　　金：We acknowledge the financial support from the National Natural Science Foundation of China(21672248 and 21621002);E-Institutes of Shanghai Municipal Education Commission(E09013);the Strategic Priority Research Program of the Chinese Academy of Sciences(XDB20020000)。

摘　　要：Summary of main observation and conclusion OSW-1 is a well-known natural saponin with potent antitumor activities.We have designed and pre-pared a small library of 22 OSW-1 analogues with a variety of p-acylamino-benzoyl groups installed at C2"of the xylose residue,wherein a regioselective(1>3)-glycosylation of arabinoside 3,4-diol has been achieved by manipulatian of the protecting groups on the imidate donors.Bioassays lead to new structure-activity relationships as well as two aplicable fluorescent probes,which are found to localize to lysosomes in HeLa cells and could be used in further antitumor mechanism studies of OSW-1 in living cells.

关 键 词：BENZOYL ANALOGUES CONCLUSION 

分 类 号：O62[理学—有机化学]