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

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

    Research output: Contribution to journalArticlepeer-review

    34 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

    Keywords

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

    ASJC Scopus subject areas

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

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