Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of hydroxylated 2,4-diphenyl-6-aryl pyridines

Radha Karki, Pritam Thapa, Mi Jeong Kang, Tae Cheon Jeong, Jung Min Nam, Hye Lin Kim, Younghwa Na, Won Jea Cho, Youngjoo Kwon, Eung Seok Lee

Research output: Contribution to journalArticlepeer-review

92 Scopus citations

Abstract

A new series of 2,4-diphenyl-6-aryl pyridines containing hydroxyl group(s) at the ortho, meta, or para position of the phenyl ring were synthesized, and evaluated for topoisomerase I and II inhibitory activity and cytotoxicity against several human cancer cell lines for the development of novel anticancer agents. Structure-activity relationship study revealed that the substitution of hydroxyl group(s) increased topoisomerase I and II inhibitory activity in the order of meta > para > ortho position. Substitution of hydroxyl group on the para position showed better cytotoxicity.

Original languageEnglish
Pages (from-to)3066-3077
Number of pages12
JournalBioorganic and Medicinal Chemistry
Volume18
Issue number9
DOIs
StatePublished - 1 May 2010

Keywords

  • Anticancer agents
  • Cytotoxicity
  • Hydroxylated 2,4-diphenyl-6-aryl pyridines
  • Topoisomerase I and II inhibitor

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