Synthesis and anticancer activities of 6-amino amonafide derivatives.

Journal article

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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Authors: Norton, J; Witschi, M; Luong, L; Kawamura, A; Ghosh, S

• Publication status: Published
• Journal: Anti-cancer drugs
• Volume: 19
• Issue: 1
• Pages: 23-36
• Publication date: 2008-01-01
• DOI: 10.1097/cad.0b013e3282f00e17
• EISSN: 1473-5741
• ISSN: 0959-4973
• Language: English
• Keywords: Cell Proliferation; Antineoplastic Agents; Naphthalimides; Humans; Topoisomerase I Inhibitors; Subcellular Fractions; Imides; Acetylation; Intercalating Agents; Magnetic Resonance Spectroscopy; Neoplasm Invasiveness; Cell Line, Tumor; Isoquinolines; Cell Nucleolus; Animals; DNA; DNA Damage; Arylamine N-Acetyltransferase; Structure-Activity Relationship