Synthesis of Olaparib Derivatives and Their Antitumor Activities  

作　　者：LOU Xi-yu YANG Xuan DING Yi-li WANG Jian-jun YAN Qing-yan HUANG Xian-gui GUO Yang-hui WANG Xiang-jing XIANG Wen-sheng 

机构地区：[1]Department of Biochemical Engineering, Northeast Agricultural University, Harbin 150030, P. R. China [2]Zhejiang Hisun Pharmaceutical Co., Ltd., Taizhou 318000, P R. China

出　　处：《Chemical Research in Chinese Universities》2013年第2期231-235,共5页高等学校化学研究（英文版）

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（BRCAl/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 BRCAl-deficient cell line HCC1937.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（BRCAl/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 BRCAl-deficient cell line HCC1937.

关 键 词：Olaparib derivative BRCA 1/2 Antitumor activity 

分 类 号：TQ463.5[化学工程—制药化工] O636.1[理学—高分子化学]