The quinobenzoxazines: Relationship between DNA binding and biological activity

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

The quinobenzoxazines: Relationship between DNA binding and biological activity

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

Research output: Contribution to journal › Article › peer-review

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 language	English (US)
Pages (from-to)	443-450
Number of pages	8
Journal	Anti-Cancer Drug Design
Volume	14
Issue number	5
State	Published - Oct 1999
Externally published	Yes

Keywords

Antitumor activity
Quinobenzoxazine
Topoisomerase II

ASJC Scopus subject areas

Biochemistry
Oncology
General Biochemistry, Genetics and Molecular Biology
Pharmacology
Drug Discovery
Organic Chemistry

Cite this

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author = "Yan Kwok and Daekyu Sun and Clement, {Jacob J.} and Hurley, {Laurence H.}",

year = "1999",

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language = "English (US)",

volume = "14",

pages = "443--450",

journal = "Anti-Cancer Drug Design",

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T2 - Relationship between DNA binding and biological activity

AU - Kwok, Yan

AU - Sun, Daekyu

AU - Clement, Jacob J.

AU - Hurley, Laurence H.

PY - 1999/10

Y1 - 1999/10

N2 - 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.

AB - 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.

KW - Antitumor activity

KW - Quinobenzoxazine

KW - Topoisomerase II

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JF - Anti-Cancer Drug Design

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ER -

The quinobenzoxazines: Relationship between DNA binding and biological activity

Abstract

Keywords

ASJC Scopus subject areas

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