Design, synthesis and docking study of 5-amino substituted indeno[1,2-c]isoquinolines as novel topoisomerase i inhibitors

Daulat Bikram Khadka, Quynh Manh Le, Su Hui Yang, Hue Thi My Van, Thanh Nguyen Le, Suk Hee Cho, Youngjoo Kwon, Kyung Tae Lee, Eung Seok Lee, Won Jea Cho

Research output: Contribution to journalArticlepeer-review

15 Scopus citations

Abstract

Various 5-amino group-substituted indeno[1,2-c]isoquinolines 7a-f were synthesized based on the previous QSAR study as rigid structures of 3-arylisoquinolines. Amino group-substituted compounds, especially 5-piperazinyl indeno[1,2-c]isoquinoline 7f, displayed potent topoisomerase I inhibitory activity as well as cytotoxicities against five different tumor cell lines. A Surflex-Dock docking model of 7f was also studied.

Original languageEnglish
Pages (from-to)1924-1929
Number of pages6
JournalBioorganic and Medicinal Chemistry
Volume19
Issue number6
DOIs
StatePublished - 15 Mar 2011

Bibliographical note

Funding Information:
This work was supported by Korea Research Foundation grant ( KRF-2009-0071379 ).

Keywords

  • Cytotoxicity
  • Docking study
  • Indeno[1,2-c]isoquinolines
  • Topoisomerase I

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