2-Chlorophenyl-substituted benzofuro[3,2-b]pyridines with enhanced topoisomerase inhibitory activity: The role of the chlorine substituent

Til Bahadur Thapa Magar, Tara Man Kadayat, Hwa Jong Lee, Seojeong Park, Ganesh Bist, Aarajana Shrestha, Youngjoo Kwon, Eung Seok Lee

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19 Scopus citations

Abstract

A new series of 2-chloropheny-substituted benzofuro[3,2-b]pyridines were designed, synthesized, and evaluated for topoisomerase I and II inhibition and antiproliferative activity. Compounds 17–19, 23, 24, 26, and 27 exhibited excellent topo II inhibitory activity. A systematic structure-activity relationship study revealed the important role of chlorine substitution in the strong topoisomerase inhibitory activity.

Original languageEnglish
Pages (from-to)3279-3283
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume27
Issue number15
DOIs
StatePublished - 2017

Bibliographical note

Publisher Copyright:
© 2017 Elsevier Ltd

Keywords

  • Antiproliferative activity
  • Benzofuro[3,2-b]pyridines
  • Chlorine-substituent
  • Heterocycles
  • Topoisomerase I and II inhibition

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