Synthesis of N-substituted 5-[2-(N-alkylamino)ethyl]dibenzo[c,h][1,6]naphthyridines as novel topoisomerase I-targeting antitumor agents

Wei Feng, Mavurapu Satyanarayana, Liang Cheng, Angela Liu, Yuan Chin Tsai, Leroy F. Liu, Edmond J. LaVoie

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

Several N-alkyl and N,N-dialkyl 5H-8,9-dimethoxy-5-(2-aminoethyl)-2,3-methylenedioxydibenzo[c,h][1,6]naphthyridin-6-ones have been identified as topoisomerase I-targeting agents with potent antitumor activity. In the present study, the impact on biological activity of substitution of a trifluoromethyl, cyano, aminocarbonyl, or ethynyl group on a N-methyl substituent of N,N-dimethyl-, N-methyl-N-ethyl-, and N-methyl-N-isopropyl 5H-8,9-dimethoxy-5-(2-aminoethyl)-2,3-methylenedioxydibenzo[c,h][1,6]naphthyridin-6-ones was assessed.

Original languageEnglish
Pages (from-to)9295-9301
Number of pages7
JournalBioorganic and Medicinal Chemistry
Volume16
Issue number20
DOIs
Publication statusPublished - Oct 15 2008
Externally publishedYes

Fingerprint

Naphthyridines
Type I DNA Topoisomerase
Bioactivity
Antineoplastic Agents
Substitution reactions

Keywords

  • Antitumor
  • Cytotoxicity
  • MDA-MB-435
  • Non-camptothecin
  • Structure-activity
  • Topoisomerase I

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

Cite this

Synthesis of N-substituted 5-[2-(N-alkylamino)ethyl]dibenzo[c,h][1,6]naphthyridines as novel topoisomerase I-targeting antitumor agents. / Feng, Wei; Satyanarayana, Mavurapu; Cheng, Liang; Liu, Angela; Tsai, Yuan Chin; Liu, Leroy F.; LaVoie, Edmond J.

In: Bioorganic and Medicinal Chemistry, Vol. 16, No. 20, 15.10.2008, p. 9295-9301.

Research output: Contribution to journalArticle

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AU - Feng, Wei

AU - Satyanarayana, Mavurapu

AU - Cheng, Liang

AU - Liu, Angela

AU - Tsai, Yuan Chin

AU - Liu, Leroy F.

AU - LaVoie, Edmond J.

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