AQ4N: an alkylaminoanthraquinone N-oxide showing bioreductive potential and positive interaction with radiation in vivo.

@article{McKeown1995AQ4NAA,
  title={AQ4N: an alkylaminoanthraquinone N-oxide showing bioreductive potential and positive interaction with radiation in vivo.},
  author={S. McKeown and M. Hejmadi and I. A. McIntyre and J. McAleer and L. H. Patterson},
  journal={British Journal of Cancer},
  year={1995},
  volume={72},
  pages={76 - 81}
}
AQ4N (1,4-bis([2-(dimethylamino-N-oxide)ethyl]amino)5,8-dihydroxy- anthracene-9,10-dione) is a novel alkylaminoanthraquinone N-oxide which, on reduction, forms a stable DNA affinic cytotoxic compound AQ4. The in vivo anti-tumour efficacy of AQ4N was investigated in B6D2F1 mice bearing the T50/80 mammary carcinoma. The effect of the drug was evaluated in combination with hypobaric hypoxia and with radiation (single and multiple fractions). Systemic toxicity was assessed by weight loss post… Expand
DNA topoisomerase II-dependent cytotoxicity of alkylaminoanthraquinones and their N-oxides
TLDR
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A combination of assays has shown that AQ4N possesses antiangiogenic effects in normoxic conditions, which could potentially contribute to antitumor activity. Expand
Evaluation of theAntiangiogenic Potential of AQ4N
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The kinetics of the expression of the DNA damage is consistent with this hypothesis and shows that AQ4 has persistent activity in vivo. Expand
A large-scale synthesis of the bioreductive drug 1,4-bis{[2-(dimethylamino)ethyl]amino}-5,8-dihydroxyanthracene-9,10-dione bis-N-oxide (AQ4N)
A large-scale synthesis of the bis-bioreductive drug 1,4-bis{[2-(dimethylamino)ethyl]amino}-5,8-dihydroxyanthracene-9,10-dione bis-N-oxide (AQ4N) has been developed. This six-step synthesis providesExpand
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TLDR
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AQ4N has the potential to improve the clinical efficacy of cisplatin and to compare it to the chemopotentiation effect of tirapazamine. Expand
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This is the first demonstration that CYPs alone can be used in a GDEPT strategy for bioreduction of the cytotoxic prodrug, AQ4N, which is the only CYP-activated bioreductive agent in clinical trials. Expand
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