Synthesis of 2-(thienyl-2-yl or -3-yl)-4-furyl-6-aryl pyridine derivatives and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship

Pritam Thapa, Radha Karki, Hoyoung Choi, Jae Hun Choi, Minho Yun, Byeong Seon Jeong, Mi Ja Jung, Jung Min Nam, Younghwa Na, Won Jea Cho, Youngjoo Kwon, Eung Seok Lee

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Abstract

A series of 2-(thienyl-2-yl or -3-yl)-4-furyl-6-aryl pyridine derivatives were designed, synthesized, and evaluated for their topoisomerase I and II inhibition and cytotoxic activity against several human cancer cell lines. Compounds 10-19 showed moderate topoisomerase I and II inhibitory activity and 20-29 showed significant topoisomerase II inhibitory activity. Structure-activity relationship study revealed that 4-(5-chlorofuran-2-yl)-2-(thiophen-3-yl) moiety has an important role in displaying topoisomerase II inhibition.

Original languageEnglish
Pages (from-to)2245-2254
Number of pages10
JournalBioorganic and Medicinal Chemistry
Volume18
Issue number6
DOIs
StatePublished - 15 Mar 2010

Keywords

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

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