Topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of dihydroxylated 2,6-diphenyl-4-aryl pyridines

Radha Karki, Chanju Song, Tara Man Kadayat, Til Bahadur Thapa Magar, Ganesh Bist, Aarajana Shrestha, Younghwa Na, Youngjoo Kwon, Eung Seok Lee

Research output: Contribution to journalArticlepeer-review

25 Scopus citations

Abstract

Abstract A new series of thirty-six dihydroxylated 2,6-diphenyl-4-aryl pyridines containing hydroxyl groups at the ortho, meta, or para position of 2- and 6-phenyl rings attached to the central pyridine were designed and synthesized. They were evaluated for topoisomerase I and II inhibitory activity and cytotoxicity against several human cancer cell lines for the development of novel anticancer agents. Most of the compounds with hydroxyl moiety either at the meta or para position of 2- or 6-phenyl ring in combination with thienyl or furyl group at 4-position of central pyridine displayed significant topoisomerase II inhibitory activity and cytotoxicity. Positive correlation between topoisomerase II inhibitory activity and cytotoxicity was observed for the compounds 9-11, 15-17, 19, 21-23, 28, and 41. Among all the synthesized compounds, compound 17 emerged as the most promising topoisomerase II inhibitor with significant cytotoxicity.

Original languageEnglish
Article number12214
Pages (from-to)3638-3654
Number of pages17
JournalBioorganic and Medicinal Chemistry
Volume23
Issue number13
DOIs
StatePublished - 2015

Keywords

  • Anticancer agents
  • Cytotoxicity
  • Dihydroxylated 2,6-diphenyl-4-aryl pyridines
  • Topoisomerase I
  • Topoisomerase II

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