Abstract
We have designed and synthesized several structural isomers of anthramycin (heterocycles 2, 3, 5, 6, and 8) and found that, in particular, pyrrolobenzodiazepine 8 induces DNA cleavage and formation of small fragments of DNA. The cytotoxic effects of 8 were manifested with both non-transformed primary neuronal/glial cells and transformed Jurkat cells. The other compounds did not change the viability either of transformed or of non-transformed cells, and induced DNA cleavage to a lesser extent.
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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Cell Survival / drug effects
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Cells, Cultured
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DNA / drug effects
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DNA / metabolism
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Humans
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Jurkat Cells
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Leukemia, T-Cell / drug therapy*
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Leukemia, T-Cell / pathology
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Neuroglia / drug effects*
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Neurons / drug effects*
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Benzodiazepines
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DNA