Abstract
A series of novel C2-exo unsaturated pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) has been synthesised via a versatile pro-C2 ketone precursor. C2-exo-unsaturation enhances both DNA-binding reactivity and in vitro cytotoxic potency.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antibiotics, Antineoplastic / chemistry*
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Antibiotics, Antineoplastic / metabolism
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Antibiotics, Antineoplastic / pharmacology
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Benzodiazepines / chemistry*
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Benzodiazepines / metabolism
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Benzodiazepines / pharmacology
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Benzodiazepinones / chemistry
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DNA / metabolism*
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Drug Screening Assays, Antitumor
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Female
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Humans
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Molecular Structure
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Ovarian Neoplasms
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Pyrroles / chemistry*
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Pyrroles / metabolism
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Pyrroles / pharmacology
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Tumor Cells, Cultured
Substances
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Antibiotics, Antineoplastic
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Benzodiazepinones
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Pyrroles
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Benzodiazepines
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tomaymycin
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DNA