Abstract
A new class of C8-linked pyrrolo[2,1-c][1,4]benzodiazepine-chalcone conjugates have been prepared by employing a solid-phase synthetic protocol. In this strategy an intramolecular aza-Wittig reductive cyclization approach has been utilized. Interestingly, some of these molecules have shown enhanced DNA-binding affinity and promising anticancer activity on a large number of human cancer cell lines.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology*
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Benzodiazepines / chemical synthesis
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Benzodiazepines / pharmacology*
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Binding Sites
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Cell Line, Tumor / drug effects*
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Chalcone / analogs & derivatives
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Chalcone / chemical synthesis
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Chalcone / pharmacology*
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DNA / chemistry
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DNA / metabolism*
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Drug Screening Assays, Antitumor
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Humans
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Models, Chemical
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Pyrroles / chemical synthesis
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Pyrroles / pharmacology*
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Pyrroles
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pyrrolo(2,1-c)(1,4)benzodiazepine
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Benzodiazepines
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Chalcone
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DNA