2. Academic Validation
  3. Synthesis of cholestane glycosides bearing OSW-1 disaccharide or its 1-->4-linked analogue and their antitumor activities

Synthesis of cholestane glycosides bearing OSW-1 disaccharide or its 1-->4-linked analogue and their antitumor activities

  • Bioorg Med Chem Lett. 2010 Sep 15;20(18):5439-42. doi: 10.1016/j.bmcl.2010.07.085.
Dan Zheng 1,  Liang Zhou,  Yuyao Guan,  Xiaozhuo Chen,  Wanqi Zhou,  Xiaoguang Chen,  Pingsheng Lei
Affiliations

Affiliation

  • 1 Key Laboratory of Bioactivity Substance and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Materia Medica, Department of Pharmacology, Peking Union Medical College & Chinese Academy of Medical Sciences, Peking 100050, PR China.
PMID: 20719510 DOI: 10.1016/j.bmcl.2010.07.085
Abstract

For further structure-activity relationship (SAR) research of OSW saponins, a cholestane glycoside, namely 3beta, 16beta, 26-trihydroxycholest-5-en-22-one 16-O-(2-O-4-methoxybenzoyl-beta-D-xylopyranosyl)-(1-->3)-2-O-acetyl-alpha-L-arabinopyranoside (1) together with two 1-->4-linked disaccharide analogues (2 and 3) were synthesized. Their cytotoxic activities were evaluated by the standard MTT assay. Compound 1 showed potent cytotoxicity against five types of human tumor cells, with IC50 ranging between 1.3 and 73 nM.

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