Synthesis and antitumor activity of des-AB analogue of steroidal saponin OSW-1

• DOI: 10.1016/j.tet.2013.06.105
• Publication Date: 2013-07-04T13:01:09Z
• Authors: Daishiro Minato; Bozhi Li; Dejun Zhou; Yasumi Shigeta; Naoki Toyooka; Hiroaki Sakurai; Kenji Sugimoto; Hideo Nemoto; Yuji Matsuya
• Keywords: 01 natural sciences; 3. Good health; 0104 chemical sciences

Abstract Simplified des-AB-type aglycone of antitumor steroidal saponin OSW-1 was concisely prepared starting from readily available Hajos ketone. We further completed the synthesis of des-AB-OSW-1 analogue by the installation of the disaccharide moiety into the des-AB aglycone, and evaluated its antitumor activity. The results indicated that a truncated aglycone drug design strategy based on OSW-1 would be a promising approach for the development of novel antitumor agents.