高等学校化学学报

高等学校化学学报 ›› 1998, Vol. 19 ›› Issue (2): 243.

• 研究快报 • 上一篇    下一篇

抗癌药物放线菌素D类似物的全合成及生物活性研究

倪京满1, 王锐2, 贾正平2, 潘鑫复1, 胡晓愚2   

  1. 1. 兰州大学生物系, 化学系;
    2. 应用有机化学国家重点实验室, 兰州, 730000
  • 收稿日期:1997-07-04 出版日期:1998-02-24 发布日期:1998-02-24
  • 通讯作者: 王锐
  • 作者简介:倪京满,女,32岁,博士研究生.
  • 基金资助:

    国家自然科学基金(批准号:29502007)、国家教委优秀年轻教师基金、博士点基金和霍英东教育基金资助课题.

Studies on the Synthesis and Bioactivity of 5,5'-Val2-AMD and 2,2'-Phe2-AMD

NI Jing-Man1, WANG Rui2, JIA Zheng-Ping2, PAN Xin-Fu1, HU Xiao-Yu2   

  1. 1. Department of Biology, Department of Chemistry;
    2. State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou, 730000
  • Received:1997-07-04 Online:1998-02-24 Published:1998-02-24

PDF (PC)

被引次数

22

关键词: 合成, 生物活性, 5, 5'-双缬氨酸放线菌素D, 2, 2'-双苯丙氨酸放线菌素D

Abstract: A ctinomycin D(AMD) contains a planar phenorazone ring as well as two cyclic depsipeptides and is best known for its effectiveness as an inhibitor of transcription. It has been used clinically for treating Wilm's tumor, gestational chriocarcinoma. Although it possesses valuable biological activities its high cytotoxity and inactivities toward some tumors have prompted the search for modified AMD. On the basis of the result of AMD-DNA binding model proposed by Takusagawa, we designed and synthesized 5,5'-Val2-AMD and 2,2'-Phe2AMD. The title compounds were synthesized from 3 in 13 steps with overall yield of 27%, 17%, respectively. The structures were identified with 1H NMR, 2D NMR, MS and HRMS. The biological activities of two analogs were carried out in comparison with those of AMD. The order of antitumor activity was 2,2'-Phe2-AMD>AMD>5,5'-Val2-AMD.

Key words: Synthesis, Bioactivity, 5,5'-Val2-AMD, 2,2'-Phe2-AMD

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