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

H. T M Van, Quynh Manh Le, Kwang Youl Lee, Eung Seok Lee, Youngjoo Kwon, Tae Sung Kim, Thanh Nguyen Le, Suh H. Lee, Won J. Cho

Research output: Contribution to journalArticle

29 Citations (Scopus)

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-ibutoxy 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.

Original languageEnglish
Pages (from-to)5763-5767
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number21
DOIs
Publication statusPublished - 2007 Nov 1

Fingerprint

Isoquinolines
Topoisomerase I Inhibitors
Type I DNA Topoisomerase
Cyclization
Cytotoxicity
Tumor Cell Line
Tumors
Cells
In Vitro Techniques

Keywords

  • Antitumor agents
  • Cytotoxicity
  • Docking study
  • Indenoisoquinoline
  • Synthesis
  • Topoisomerase 1

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

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. / Van, H. T M; Le, Quynh Manh; Lee, Kwang Youl; Lee, Eung Seok; Kwon, Youngjoo; Kim, Tae Sung; Le, Thanh Nguyen; Lee, Suh H.; Cho, Won J.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 17, No. 21, 01.11.2007, p. 5763-5767.

Research output: Contribution to journalArticle

Van, H. T M ; Le, Quynh Manh ; Lee, Kwang Youl ; Lee, Eung Seok ; Kwon, Youngjoo ; Kim, Tae Sung ; Le, Thanh Nguyen ; Lee, Suh H. ; Cho, Won J. / 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. In: Bioorganic and Medicinal Chemistry Letters. 2007 ; Vol. 17, No. 21. pp. 5763-5767.
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