Abstract
In the context of the design and synthesis of minor groove binding and intercalating DNA ligands some new oligopyrrole carboxamides were synthesized. These hybrid molecules (combilexins) possess a variable and conformatively flexible spacer at the N-terminal end. As intercalating tricyclic systems acridone, acridine, anthraquinones and in a special case iminostilbene terminate the N-terminal end of the pyrrole chain. The cytotoxicity was examined by the NCI antitumor screening, furthermore, biophysical as well as biochemical studies were performed in order to get some information about the DNA binding properties and topoisomerase inhibition effect of this new series of molecules.
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 / chemistry
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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DNA / chemistry
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DNA / metabolism*
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DNA Footprinting
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Distamycins / chemical synthesis
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Distamycins / chemistry
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Distamycins / pharmacology*
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Drug Design*
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Humans
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Intercalating Agents / chemistry*
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Ligands
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Molecular Structure
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Netropsin / chemical synthesis
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Netropsin / chemistry
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Netropsin / pharmacology*
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Pyrroles / chemical synthesis
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Pyrroles / chemistry
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Pyrroles / pharmacology
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Structure-Activity Relationship
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Topoisomerase Inhibitors*
Substances
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Antineoplastic Agents
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Distamycins
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Intercalating Agents
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Ligands
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Pyrroles
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Topoisomerase Inhibitors
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Netropsin
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stallimycin
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DNA