Synthesis of 1-(ω-aminoalkyl)naphthoindolediones with antiproliferative properties

The preparation and cytotoxic properties of N-aminoalkyl-4,11-dihydroxynaphtho[2,3- f]indole-5,10-diones are described. The N-aminobutylnaphthoindolediones are less active in vitro against the majority of human cancer cell lines, but have higher potency than adriamycin or mitoxantrone against adriam...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2004-07, Vol.12 (14), p.3923-3930
Main Authors: Shchekotikhin, Andrey E, Buyanov, Vladimir N, Preobrazhenskaya, Maria N
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Cell Division - drug effects
Cell Line, Tumor
Cytotoxicity
Drug Screening Assays, Antitumor
Humans
N-Alkylation
Naphthoindolediones
Naphthols - chemical synthesis
Naphthols - pharmacology
O-Demethylation
Spectrum Analysis
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Summary:The preparation and cytotoxic properties of N-aminoalkyl-4,11-dihydroxynaphtho[2,3- f]indole-5,10-diones are described. The N-aminobutylnaphthoindolediones are less active in vitro against the majority of human cancer cell lines, but have higher potency than adriamycin or mitoxantrone against adriamycin resistant breast cancer cell line NCI/ADR. The preparation and cytotoxic properties of 4,11-dihydroxynaphtho[2,3- f]indole-5,10-dione derivatives carrying N-aminoalkyl substituents are described. The N-aminobutylnaphthoindolediones obtained were studied in National Cancer Institute Screening Program and demonstrated high antiproliferative activity against 60 human cancer cell lines. All N-(4-aminobutyl) derivatives have higher potency than adriamycin or mitoxantrone against adriamycin selected multidrug resistant breast cancer cell line NCI/ADR.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2004.04.042