Design, synthesis, and evaluation of a novel pyrrolobenzodiazepine DNA-interactive agent with highly efficient cross-linking ability and potent cytotoxicity

A novel sequence-selective pyrrolobenzodiazepine (PBD) dimer 5 (SJG-136) has been developed that comprises two C2-exo-methylene-substituted DC-81 (3) subunits tethered through their C8 positions via an inert propanedioxy linker. This symmetric molecule is a highly efficient minor groove interstrand...

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Veröffentlicht in:	Journal of medicinal chemistry Jg. 44; H. 5; S. 737
Hauptverfasser:	Gregson, S J, Howard, P W, Hartley, J A, Brooks, N A, Adams, L J, Jenkins, T C, Kelland, L R, Thurston, D E
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	United States 01.03.2001
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Benzodiazepinones - chemical synthesis Benzodiazepinones - chemistry Benzodiazepinones - pharmacology Cisplatin - pharmacology Cross-Linking Reagents - chemical synthesis Cross-Linking Reagents - chemistry Cross-Linking Reagents - pharmacology DNA - chemistry Drug Design Drug Resistance, Neoplasm Drug Screening Assays, Antitumor Electrophoresis, Agar Gel Heating Humans Models, Molecular Protein Denaturation Pyrroles - chemical synthesis Pyrroles - chemistry Pyrroles - pharmacology Structure-Activity Relationship Tumor Cells, Cultured
ISSN:	0022-2623
Online-Zugang:	Weitere Angaben
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