新型3-芳基异喹啉胺的合成：对拓扑异构酶I抑制作用及细胞毒性的影响
Synthesis of new 3-arylisoquinolinamines: effect on topoisomerase I inhibition and cytotoxicity.
作者信息
Cho Won-Jea, Min Sun Young, Le Thanh Nguyen, Kim Tae Sung
机构信息
College of Pharmacy, Chonnam National University, Yong-Bong dong, Buk-gu, Kwangju 500-757, South Korea.
出版信息
Bioorg Med Chem Lett. 2003 Dec 15;13(24):4451-4. doi: 10.1016/j.bmcl.2003.09.001.
PMID:14643344
Abstract
To investigate the structure-activity relationships of 3-arylisoquinolines, diverse substituted 3-aryisoquinolinamines were synthesized and tested in vitro antitumor activity against four tumor cell lines. Some of the compounds showed potent topoisomerase I inhibitory activity. Docking study of 7d with topoisomerase I-DNA complex was also performed.
摘要
为研究3-芳基异喹啉的构效关系，合成了多种取代的3-芳基异喹啉胺，并对四种肿瘤细胞系进行了体外抗肿瘤活性测试。部分化合物表现出较强的拓扑异构酶I抑制活性。还对化合物7d与拓扑异构酶I-DNA复合物进行了对接研究。
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