The quinobenzoxazines: Relationship between DNA binding and biological activity

Yan Kwok, Daekyu Sun, Jacob J. Clement, Laurence Hurley

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

The quinobenzoxazine compounds, derived from antibacterial quinolones, is active in vitro and in vivo against murine and human tumors. In this contribution, we show that the relative DNA binding affinity of the quinobenzoxazine compounds correlates with their cytotoxicity, their ability to inhibit gyrase-DNA complex formation, and the decatenation of kinetoplast DNA by human topoisomerase II. DNA binding studies with the descarboxy-A-62176 analogue indicate that the β-keto acid moiety of the quinobenzoxazine compounds plays an important role in their interaction with DNA.

Original languageEnglish (US)
Pages (from-to)443-450
Number of pages8
JournalAnti-Cancer Drug Design
Volume14
Issue number5
StatePublished - Oct 1999
Externally publishedYes

Fingerprint

Bioactivity
A 62176
DNA
Kinetoplast DNA
DNA Gyrase
Keto Acids
Type II DNA Topoisomerase
Quinolones
Cytotoxicity
Tumors
Neoplasms

Keywords

  • Antitumor activity
  • Quinobenzoxazine
  • Topoisomerase II

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Oncology
  • Biochemistry, Genetics and Molecular Biology(all)
  • Biochemistry
  • Pharmacology

Cite this

The quinobenzoxazines : Relationship between DNA binding and biological activity. / Kwok, Yan; Sun, Daekyu; Clement, Jacob J.; Hurley, Laurence.

In: Anti-Cancer Drug Design, Vol. 14, No. 5, 10.1999, p. 443-450.

Research output: Contribution to journalArticle

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