Cytotoxicity and TOP1-targeting activity of 8- and 9-amino derivatives of 5-butyl- and 5-(2-N,N-dimethylamino)ethyl-5H-dibenzo[c,h][1,6]naphthyridin-6-ones

Lisa Sharma, Yuan Chin Tsai, Angela A. Liu, Leroy F. Liu, Edmond J. LaVoie

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

Studies on substituted 5H-dibenzo[c,h][1,6]naphthyridin-6-ones and 6H-dibenzo[c,h][2,6]naphthyridin-5-ones have demonstrated that hydrophilic substituents at the 2-position of an ethyl group at the 5- and 6-positions, respectively, can enhance biological activity. The compatibility of such hydrophilic groups at other sites with either TOP1-targeting activity or potent cytotoxic activity has not been explored. The present study examines the influence on biological activity of either a 2-(N,N-dimethylamino)ethyl or a N,N-dimethylacetamide derivative of 8- or 9-amino-5H-dibenzo[c,h]naphthyridin-6-ones that have a 5-butyl- or 5-[2-(N,N-dimethylamino)ethyl]-substituent.

Original languageEnglish
Pages (from-to)1471-1476
Number of pages6
JournalEuropean Journal of Medicinal Chemistry
Volume44
Issue number4
DOIs
Publication statusPublished - Apr 2009
Externally publishedYes

    Fingerprint

Keywords

  • 5H-Dibenzo[c,h][1,6]naphthyridin-6-ones
  • Cytotoxicity
  • Multidrug resistance
  • Topoisomerase I-targeting agents

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

Cite this