2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 2007 Nov 1;17(21):5763-7. doi: 10.1016/j.bmcl.2007.08.062.
Hue Thi My Van 1,  Quynh Manh Le,  Kwang Youl Lee,  Eung-Seok Lee,  Youngjoo Kwon,  Tae Sung Kim,  Thanh Nguyen Le,  Suh-Hee Lee,  Won-Jea Cho
Affiliations

Affiliation

  • 1 College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju 500-757, Republic of Korea.
PMID: 17827007 DOI: 10.1016/j.bmcl.2007.08.062
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.

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