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高等学校化学研究 ›› 2013, Vol. 29 ›› Issue (2): 231-235.doi: 10.1007/s40242-013-2448-5

• Articles • 上一篇    下一篇

Synthesis of Olaparib Derivatives and Their Antitumor Activities

LOU Xi-yu1, YANG Xuan2, DING Yi-li2, WANG Jian-jun2, YAN Qing-yan2, HUANG Xian-gui2, GUO Yang-hui2, WANG Xiang-jing1, XIANG Wen-sheng1   

  1. 1. Department of Biochemical Engineering, Northeast Agricultural University, Harbin 150030, P. R. China;
    2. Zhejiang Hisun Pharmaceutical Co., Ltd., Taizhou 318000, P. R. China
  • 收稿日期:2012-11-20 修回日期:2013-01-07 出版日期:2013-04-01 发布日期:2013-03-20
  • 通讯作者: XIANG Wen-sheng E-mail:xiangwensheng@yahoo.com.cn
  • 基金资助:

    Supported by the National Basic Research Program of China(No.2010CB126102), the Outstanding Youth Foundation of Heilongjiang Province, China(No.JC201201) and the Program for New Teachers in University, China(No.20092325120007).

Synthesis of Olaparib Derivatives and Their Antitumor Activities

LOU Xi-yu1, YANG Xuan2, DING Yi-li2, WANG Jian-jun2, YAN Qing-yan2, HUANG Xian-gui2, GUO Yang-hui2, WANG Xiang-jing1, XIANG Wen-sheng1   

  1. 1. Department of Biochemical Engineering, Northeast Agricultural University, Harbin 150030, P. R. China;
    2. Zhejiang Hisun Pharmaceutical Co., Ltd., Taizhou 318000, P. R. China
  • Received:2012-11-20 Revised:2013-01-07 Online:2013-04-01 Published:2013-03-20
  • Supported by:

    Supported by the National Basic Research Program of China(No.2010CB126102), the Outstanding Youth Foundation of Heilongjiang Province, China(No.JC201201) and the Program for New Teachers in University, China(No.20092325120007).

摘要:

A series of Olaparib derivatives was synthesized, and their structures were confirmed by 1H NMR, MS and elemental analysis. Their antitumor activities on breast cancer susceptbility gene 1/2(BRCA1/2)-deficient cancer cell lines including HCC1937, Capan-1 and MDA-MB-436 were evaluated. The antitumor activity of compound Olaparib-1 was better than the positive control Olaparib in BRCA1-deficient cell line HCC1937.

关键词: Olaparib derivative, BRCA1/2, Antitumor activity

Abstract:

A series of Olaparib derivatives was synthesized, and their structures were confirmed by 1H NMR, MS and elemental analysis. Their antitumor activities on breast cancer susceptbility gene 1/2(BRCA1/2)-deficient cancer cell lines including HCC1937, Capan-1 and MDA-MB-436 were evaluated. The antitumor activity of compound Olaparib-1 was better than the positive control Olaparib in BRCA1-deficient cell line HCC1937.

Key words: Olaparib derivative, BRCA1/2, Antitumor activity