11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents

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

Research output: Contribution to journalArticle

10 Citations (Scopus)

Abstract

Several 11-substituted benzo[i]phenanthridine derivatives were synthesized, and their TOP1-targeting activity and cytotoxicity were assessed. Comparative data indicate that TOP1-targeting was often the primary molecular target associated with their cytotoxicity. Several 11-aminoalkyl derivatives, 11-aminocarboxy derivatives as well as the 11-[(2-dimethylamino)ethyl]carboxamide of 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine were synthesized and did exhibit considerable cytotoxicity with IC50 values ranging from 20 to 120 nM in the human lymphoblast tumor cell line RPMI8402.

Original languageEnglish
Pages (from-to)8598-8606
Number of pages9
JournalBioorganic and Medicinal Chemistry
Volume16
Issue number18
DOIs
Publication statusPublished - Sep 15 2008
Externally publishedYes

Fingerprint

Phenanthridines
Type I DNA Topoisomerase
Cytotoxicity
Derivatives
Tumor Cell Line
Inhibitory Concentration 50
Tumors
Cells

Keywords

  • Antitumor agents
  • Benzo[i]phenanthridines
  • Cytotoxicity
  • Multidrug resistance
  • Photocyclization
  • Topoisomerase I

ASJC Scopus subject areas

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

Cite this

11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents. / Feng, Wei; Satyanarayana, Mavurapu; Tsai, Yuan Chin; Liu, Angela A.; Liu, Leroy F.; LaVoie, Edmond J.

In: Bioorganic and Medicinal Chemistry, Vol. 16, No. 18, 15.09.2008, p. 8598-8606.

Research output: Contribution to journalArticle

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AU - Tsai, Yuan Chin

AU - Liu, Angela A.

AU - Liu, Leroy F.

AU - LaVoie, Edmond J.

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