[2,1-c] [1,4]Benzodiazepine (PBD)-Distamycin Hybrid Inhibits DNA Binding to Transcription Factor Sp1

We designed and synthesized the hybrid 6, prepared combining the minor groove binders distamycin A and pyrrolo [2,1-c][1,4] benzodiazepine (PBD) 4, related to the natural occurring anthramycin (2) and DC-81 (3). In this paper, the effects of the compound 6 on molecular interactions between DNA and t...

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Veröffentlicht in:	Nucleosides, nucleotides & nucleic acids nucleotides & nucleic acids, 2000-08, Vol.19 (8), p.1219-1229
Hauptverfasser:	Baraldi, P. G., Cacciarit, B., Guiotto, A., Romagnoli, R., Spalluto, G., Leoni, A., Bianchi, N., Feriotto, G., Rutigliano, C., Mischiati, C., Gambari, Roberto
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Benzodiazepinones - chemical synthesis Benzodiazepinones - chemistry Benzodiazepinones - pharmacology Burkitt Lymphoma - pathology Cell Division - drug effects Distamycins - chemical synthesis Distamycins - chemistry Distamycins - pharmacology DNA, Neoplasm - drug effects DNA, Neoplasm - metabolism Drug Screening Assays, Antitumor Gene Expression Regulation, Neoplastic - drug effects Humans K562 Cells - drug effects Leukemia L1210 - pathology Magnetic Resonance Spectroscopy Mice Sp1 Transcription Factor - antagonists & inhibitors Sp1 Transcription Factor - metabolism Transcription, Genetic - drug effects Tumor Cells, Cultured - drug effects
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Zusammenfassung:	We designed and synthesized the hybrid 6, prepared combining the minor groove binders distamycin A and pyrrolo [2,1-c][1,4] benzodiazepine (PBD) 4, related to the natural occurring anthramycin (2) and DC-81 (3). In this paper, the effects of the compound 6 on molecular interactions between DNA and transcription factor Sp1 were studied. The results obtained demonstrate that PBD-distamycin hybrid is a powerful inhibitor of Sp1/DNA interactions.
ISSN:	1525-7770 1532-2335
DOI:	10.1080/15257770008033045