The quinobenzoxazines: Relationship between DNA binding and biological activity

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

Research output: Contribution to journalArticle

9 Scopus citations

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 1 1999
Externally publishedYes

Keywords

  • Antitumor activity
  • Quinobenzoxazine
  • Topoisomerase II

ASJC Scopus subject areas

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

Fingerprint Dive into the research topics of 'The quinobenzoxazines: Relationship between DNA binding and biological activity'. Together they form a unique fingerprint.

  • Cite this