Synthesis and DNA cleavage activity of a novel bleomycin A(5) glycoconjugate

[structure in text] To explore the possibility of modifying bleomycin in a fashion that could alter its physiological distribution in a therapeutic setting, a new analogue of bleomycin has been prepared. This analogue is intended to target the asialoglycoprotein receptor on liver cells. Critically,...

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Veröffentlicht in:	Organic letters 2001-05, Vol.3 (9), p.1291-1294
Hauptverfasser:	Choudhury, A K, Tao, Z F, Hecht, S M
Format:	Artikel
Sprache:	eng
Schlagworte:	Bleomycin - analogs & derivatives Bleomycin - chemical synthesis Bleomycin - chemistry Bleomycin - pharmacology Carcinoma, Squamous Cell - drug therapy Catalysis DNA - drug effects DNA - metabolism Humans Liver - cytology Molecular Structure Plasmids - chemistry Structure-Activity Relationship Tumor Cells, Cultured - drug effects
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Zusammenfassung:	[structure in text] To explore the possibility of modifying bleomycin in a fashion that could alter its physiological distribution in a therapeutic setting, a new analogue of bleomycin has been prepared. This analogue is intended to target the asialoglycoprotein receptor on liver cells. Critically, despite the large C-substituent, the bleomycin conjugate was found to degrade DNA in the same fashion as bleomycin A(5) itself, and with only modestly decreased efficiency.
ISSN:	1523-7060
DOI:	10.1021/ol010015h