Abstract
We designed and synthesized a Py-Im polyamide seco-CBI conjugate protected by a photocleavable group and demonstrated that it was selectively activated by UV irradiation both in vitro and in vivo. Sequence-specific alkylating Py-Im polyamides containing photolabile linkers may be useful for developing novel chemical- or enzyme-activated anticancer agents and may facilitate spatiotemporal control of gene expression.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkylation
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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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Base Sequence
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Cell Line, Tumor
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Cell Proliferation / drug effects
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DNA / chemistry*
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DNA / drug effects
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Drug Screening Assays, Antitumor
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Humans
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Imidazoles / chemistry*
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Indoles / chemical synthesis
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Indoles / chemistry*
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Indoles / pharmacology
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Molecular Structure
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Photochemistry
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Pyrroles / chemical synthesis
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Pyrroles / chemistry*
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Pyrroles / pharmacology
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Stereoisomerism
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Structure-Activity Relationship
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Ultraviolet Rays*
Substances
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Antineoplastic Agents
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Imidazoles
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Indoles
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Pyrroles
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polyamide 1-(chloromethyl)-5-hydroxyl-1,2-dihydro--3H-benz(e)indole conjugate
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DNA