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Synthesis and anticancer activities of 6-amino amonafide derivatives.

Abstract:

Amonafide is a DNA intercalator and topoisomerase II inhibitor in clinical development for the treatment of neoplastic diseases. Amonafide contains a free arylamine, which causes it to be metabolized in humans by N-acetyl transferase-2 (NAT2) into a toxic form. To eliminate the NAT2 acetylation of amonafide while retaining the anticancer properties, we have synthesized nine derivatives that are structurally similar to amonafide that should not be acetylated. Eight derivatives have arylamines ...

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Publication status:
Published

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Authors


Norton, JT More by this author
Witschi, MA More by this author
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Institution:
University of Oxford
Department:
Oxford, MPLS, Chemistry, Organic Chemistry, BHF Centre of Research Excellence
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Journal:
Anti-cancer drugs
Volume:
19
Issue:
1
Pages:
23-36
Publication date:
2008-01-05
DOI:
EISSN:
1473-5741
ISSN:
0959-4973
URN:
uuid:b73d10f1-6211-41b5-9b11-142225e2bac6
Source identifiers:
289142
Local pid:
pubs:289142

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