高等学校化学学报

高等学校化学学报 ›› 1998, Vol. 19 ›› Issue (S1): 25.

• Plenary, Keynote and Invited Lectures • 上一篇    下一篇

A Total Synthesis of RA-VII

Jieping Zhu   

  1. Institut de Chimie des Substances Naturelles, CNRS, 91198 Gif-sur-Yvette, France
  • 出版日期:1998-12-31 发布日期:1998-12-31
  • 通讯作者: Jieping Zhu,e-mail:zhu@icsn.cnrs-gif.fr; fax:33-1-69077247 E-mail:zhu@icsn.cnrs-gif

A Total Synthesis of RA-VII

Jieping Zhu   

  1. Institut de Chimie des Substances Naturelles, CNRS, 91198 Gif-sur-Yvette, France
  • Online:1998-12-31 Published:1998-12-31
  • Contact: Jieping Zhu,e-mail:zhu@icsn.cnrs-gif.fr; fax:33-1-69077247 E-mail:zhu@icsn.cnrs-gif

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摘要： RA-VII (1) and related bicyclic hexapeptides, isolated from Rubiaceous plants, Rubia akame,showed potent antitumor activity and in fact, RA-VII is currently undergoing phase Ⅱ clinical trial in Japan. It inhibit protein synthesis through binding,to eukaryotic 80S ribosomes, resulting in inhibition of aminoacyl-tRNA binding formation and peptidyl-tRNA translocation. The complex molecular architecture and interesting biological activity made these compounds attractive synthetic targets.

Abstract: RA-VII (1) and related bicyclic hexapeptides, isolated from Rubiaceous plants, Rubia akame,showed potent antitumor activity and in fact, RA-VII is currently undergoing phase Ⅱ clinical trial in Japan. It inhibit protein synthesis through binding,to eukaryotic 80S ribosomes, resulting in inhibition of aminoacyl-tRNA binding formation and peptidyl-tRNA translocation. The complex molecular architecture and interesting biological activity made these compounds attractive synthetic targets.

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