Synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase i and II inhibitory activity, cytotoxicity, and structure-activity relationship

Uttam Thapa, Pritam Thapa, Radha Karki, Minho Yun, Jae Hun Choi, Yurngdong Jahng, Eunyoung Lee, Kyung Hwa Jeon, Younghwa Na, Eun Mi Ha, Won Jea Cho, Youngjoo Kwon, Eung Seok Lee

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52 Scopus citations

Abstract

Designed and synthesized were a series of 5H-chromeno[4,3-b]pyridines with substitution at 2- and 4-positions with various 5- or 6-membered heteroaromatics as antitumor agents. They were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Structure-activity relationship study showed that 2-furyl or 2-thienyl at 2- or 4-position of central pyridine is crucial in displaying topo I or II inhibitory activity and cytotoxicity.

Original languageEnglish
Pages (from-to)3201-3209
Number of pages9
JournalEuropean Journal of Medicinal Chemistry
Volume46
Issue number8
DOIs
StatePublished - Aug 2011

Keywords

  • 4-chromanone
  • Cytotoxicity
  • Terpyridine
  • Terthiophene
  • Topoisomerase I and II

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