[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
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container_end_page 1229
container_issue 8
container_start_page 1219
container_title Nucleosides, nucleotides & nucleic acids
container_volume 19
creator Baraldi, P. G.
Cacciarit, B.
Guiotto, A.
Romagnoli, R.
Spalluto, G.
Leoni, A.
Bianchi, N.
Feriotto, G.
Rutigliano, C.
Mischiati, C.
Gambari, Roberto
description 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.
doi_str_mv 10.1080/15257770008033045
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G. ; Cacciarit, B. ; Guiotto, A. ; Romagnoli, R. ; Spalluto, G. ; Leoni, A. ; Bianchi, N. ; Feriotto, G. ; Rutigliano, C. ; Mischiati, C. ; Gambari, Roberto</creator><creatorcontrib>Baraldi, P. G. ; Cacciarit, B. ; Guiotto, A. ; Romagnoli, R. ; Spalluto, G. ; Leoni, A. ; Bianchi, N. ; Feriotto, G. ; Rutigliano, C. ; Mischiati, C. ; Gambari, Roberto</creatorcontrib><description>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. 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source Taylor & Francis:Master (3349 titles); MEDLINE
subjects 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
title [2,1-c] [1,4]Benzodiazepine (PBD)-Distamycin Hybrid Inhibits DNA Binding to Transcription Factor Sp1
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