2-Thienyl-4-furyl-6-aryl pyridine derivatives: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study

Pritam Thapa, Radha Karki, Uttam Thapa, Yurngdong Jahng, Mi Ja Jung, Jung Min Nam, Younghwa Na, Youngjoo Kwon, Eung Seok Lee

Research output: Contribution to journalArticlepeer-review

59 Scopus citations

Abstract

Designed and synthesized 60 2-thienyl-4-furyl-6-aryl pyridine derivatives were evaluated for their topoisomerase I and II inhibitory activities at 20 μM and 100 μM and cytotoxicity against several human cancer cell lines. Compounds 8, 9, 11-29 showed significant topoisomerase II inhibitory activity and compounds 10 and 11 showed significant topoisomerase I inhibitory activity. Most of the compounds (7-21) possessing 2-(5-chlorothiophen-2-yl)-4-(furan-3-yl) moiety showed higher or similar cytotoxicity against HCT15 cell line as compared to standards. Most of the selected compounds displayed moderate cytotoxicity against MCF-7, HeLa, DU145, and K562 cell lines. Structure-activity relationship study revealed that 2-(5-chlorothiophen-2-yl)-4-(furan-3-yl) moiety has an important role in displaying biological activities.

Original languageEnglish
Pages (from-to)377-386
Number of pages10
JournalBioorganic and Medicinal Chemistry
Volume18
Issue number1
DOIs
StatePublished - 1 Jan 2010

Keywords

  • 2-(5-Chlorothiophen-2-yl)-4-(furan-3-yl)
  • 2-Thienyl-4-furyl-6-aryl pyridine
  • Cytotoxicity
  • Topoisomerase I and II

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