The stabilization of DNA topoisomerase II cleavable complex by mitonafide analogs

Amonafide (4-aminobenzoisoqinolinedione) and its structural analog, mitonafide 1, have been shown to stabilize topoisomerase II cleavable complexes. The position of the nitro group and structural modifications of the side chain influence the interactions between drug, enzyme, and DNA. It was shown t...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 4; no. 13; pp. 1643 - 1648
Main Authors Miller, Kelli E., Grace, James M., Macdonald, Timothy L.
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 07.07.1994
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Summary:Amonafide (4-aminobenzoisoqinolinedione) and its structural analog, mitonafide 1, have been shown to stabilize topoisomerase II cleavable complexes. The position of the nitro group and structural modifications of the side chain influence the interactions between drug, enzyme, and DNA. It was shown that the analogs with the nitro in the 5-position, as in 1, are the most potent inhibitors in this structural class. Structural analogs of mitonafide [R 1=NO 2, R 2=H, and R 3 = (CH 2) 2N(CH 3) 2] were synthesized and the position of the nitro group and structural modificatins of the side chain influence the interactions between drug, enzyme, and DNA. It was shown that the analogs with the nitro in the 5-position, as in 1, are the most potent inhibitors in this structural class.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)80582-5