Chemical Research in Chinese Universities ›› 2013, Vol. 29 ›› Issue (2): 231-235.doi: 10.1007/s40242-013-2448-5

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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).

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