Abstract
A distyryl boron dipyrromethene based photosensitiser substituted with 1,2,4,5-tetrazine and alkyne moieties was prepared. Through site-specific bioorthogonal reactions with the complementary functional tags anchored on the membrane of A431 human epidermoid carcinoma cells, this versatile photosensitiser exhibited enhanced cellular uptake and photocytotoxicity. The bioorthogonal ligation was also demonstrated in tumour-bearing nude mice.
MeSH terms
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Animals
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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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Boron Compounds / chemical synthesis
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Boron Compounds / chemistry
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Boron Compounds / pharmacology*
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Cell Survival / drug effects
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Dose-Response Relationship, Drug
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Drug Screening Assays, Antitumor
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Humans
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Mice
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Mice, Nude
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Molecular Structure
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Neoplasms, Experimental / drug therapy
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Neoplasms, Experimental / metabolism
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Neoplasms, Experimental / pathology
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Optical Imaging
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Photochemotherapy*
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Photosensitizing Agents / chemical synthesis
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Photosensitizing Agents / chemistry
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Photosensitizing Agents / pharmacology*
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Porphobilinogen / analogs & derivatives*
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Porphobilinogen / chemical synthesis
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Porphobilinogen / chemistry
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Porphobilinogen / pharmacology
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Reactive Oxygen Species / analysis
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Reactive Oxygen Species / metabolism
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Boron Compounds
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Photosensitizing Agents
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Reactive Oxygen Species
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dipyrromethene
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Porphobilinogen