中山大学学报自然科学版 ›› 2012, Vol. 51 ›› Issue (2): 63-65.

• 研究论文 • 上一篇    下一篇

抗肿瘤化合物6-溴代吲哚-3-甲醇的设计合成

陶炳志1,陈河如1,2   

  1. ( 1.暨南大学药学院中药及天然药物研究所,广东 广州 510632;2.广东省中药药效物质基础及创新药物研究重点实验室, 广东 广州 510632)
  • 收稿日期:2011-12-22 修回日期:1900-01-01 出版日期:2012-03-25 发布日期:2012-03-25
  • 通讯作者: 陈河如

Design Synthesis and Application of Anti-tumor Compound 6-Bromo-Indole-3-Carbinol

TAO Bingzhi1,CHEN Heru1,2   

  1. (1. Institute of Traditional Chinese Medicine & Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, China; 2. Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Guangzhou 510632,China)
  • Received:2011-12-22 Revised:1900-01-01 Online:2012-03-25 Published:2012-03-25

摘要:

以邻硝基甲苯为原料,通过溴化、类羟醛缩合、成环、甲酰化和还原等步骤合成6-溴代吲哚-3-甲醇,总收率26.5%,所有化合物的结构均经核磁共振谱(NMR)、质谱(ESI-MS)等方法确证。以标题化合物为结构框架,合成系列6-位取代的吲哚-3-甲醇衍生物,可获得类药性好的化合物。

关键词: 吲哚-3-甲醇, 抗肿瘤, 药物合成

Abstract: Applying o-nitrotoluent as starting material, 6-bromo-indole-3-carbinol was synthesized via multiple-step reactions including bromidation, aldollike condensation, cyclization, Vilsmeier-Haack formylation and reduction. The overall yield reaches 26.5%. The structures of all the products have been confirmed by ESI-MS and NMR. Based on the scaffold of the title compound, series of 6-substituted indole-3-carbinols can be prepared in search for the better drug-like compounds.

Key words: indole-3-carbinol, anti-tumor, pharmaceutical synthesis

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