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作为3-芳基异喹啉受限形式的茚并[1,2-c]异喹啉的便捷合成以及一种拓扑异构酶I抑制剂与DNA-拓扑异构酶I复合物的对接研究。

Convenient synthesis of indeno[1,2-c]isoquinolines as constrained forms of 3-arylisoquinolines and docking study of a topoisomerase I inhibitor into DNA-topoisomerase I complex.

作者信息

Van Hue Thi My, Le Quynh Manh, Lee Kwang Youl, Lee Eung-Seok, Kwon Youngjoo, Kim Tae Sung, Le Thanh Nguyen, Lee Suh-Hee, Cho Won-Jea

机构信息

College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju 500-757, Republic of Korea.

出版信息

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5763-7. doi: 10.1016/j.bmcl.2007.08.062. Epub 2007 Aug 29.

DOI:10.1016/j.bmcl.2007.08.062
PMID:17827007
Abstract

11-hydroxyindeno[1,2-c]isoquinolines 12a-c were prepared as constrained forms of 3-arylisoquinolines through an intramolecular cyclization reaction. Among the synthesized compounds, the 11-(i)butoxy analog 15l displayed potent in vitro cytotoxicity against four different tumor cell lines as well as topoisomerase 1 inhibitory activity. A FlexX docking study was performed to explain the topoisomerase 1 activity of 15l.

摘要

通过分子内环化反应制备了11-羟基茚并[1,2-c]异喹啉12a-c，作为3-芳基异喹啉的受限形式。在合成的化合物中，11-(异)丁氧基类似物15l对四种不同的肿瘤细胞系显示出强大的体外细胞毒性以及拓扑异构酶1抑制活性。进行了FlexX对接研究以解释15l的拓扑异构酶1活性。

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