Hydroxylated 2,4-diphenyl indenopyridine derivatives as a selective non-intercalative topoisomerase catalytic inhibitor

Tara Man Kadayat, Chanmi Park, Kyu Yeon Jun, Til Bahadur Thapa Magar, Ganesh Bist, Han Young Yoo, Youngjoo Kwon, Eung Seok Lee

Research output: Contribution to journalArticlepeer-review

33 Scopus citations


For the development of novel anticancer agents, we designed and synthesized hydroxylated 2,4-diphenyl indenopyridines, and evaluated their topoisomerase inhibitory activity as well as their antiproliferative activities against several human cancer cell lines. The structure-activity relationship study showed that indenopyridines with hydroxyl group at meta or para positions of 2-or 4-phenyl ring displayed selective and significant topoisomerase IIα (topo IIα) inhibitory activity and potent antiproliferative activity. Positive correlation between topo IIα inhibition and antiproliferative activity was observed for compounds 15, 16, 18-20, 22, 23, 25 and 26. The mode of action of compound 16 was further evaluated to be a non-intercalativetopo IIα catalytic inhibitor.

Original languageEnglish
Pages (from-to)302-314
Number of pages13
JournalEuropean Journal of Medicinal Chemistry
StatePublished - Jan 2015

Bibliographical note

Funding Information:
This research was supported by the Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology ( NRF-2012R1A2A2A01046188 ).

Publisher Copyright:
© 2014 Elsevier Masson SAS.


  • Anticancer agents
  • Hydroxylated 2,4-diphenyl indenopyridine
  • Terpyridine
  • Topoisomerase IIa non-intercalative
  • catalytic inhibitorAntiproliferative activity


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