2,4-Diaryl-5,6-dihydro-1,10-phenanthroline and 2,4-diaryl-5,6- dihydrothieno[2,3-h] quinoline derivatives for topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship study

Pritam Thapa, Radha Karki, Han Young Yoo, Pil Hoon Park, Eunyoung Lee, Kyung Hwa Jeon, Younghwa Na, Won Jea Cho, Youngjoo Kwon, Eung Seok Lee

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23 Scopus citations

Abstract

Designed and synthesized thirty-two 2,4-diaryl-5,6-dihydro-1,10- phenanthroline and 2,4-diaryl-5,6-dihydrothieno[2,3-h] quinoline derivatives as rigid analogs of 2,4,6-trisubstituted pyridines were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Structure-activity relationship study showed that [2,2′;6′,2″]-terpyridine skeleton is important for the cytotoxicity against several human cancer cell lines.

Original languageEnglish
Pages (from-to)67-78
Number of pages12
JournalBioorganic Chemistry
Volume40
Issue number1
DOIs
StatePublished - Feb 2012

Bibliographical note

Funding Information:
This work was supported by the 2011 Yeungnam University Research Grant.

Keywords

  • 2,4-Diaryl-5,6- dihydrothieno[2,3-h] quinoline
  • 2,4-Diaryl-5,6-dihydro-1,10-phenanthroline
  • Cytotoxicity
  • Terpyridine
  • Topoisomerase I and II

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