Abstract
A new family of antitumor prodrugs (1-3) of 5-fluorouracil (5-FU) possessing photolabile 2-nitrobenzyl chromophores have been designed and synthesized to investigate the efficiency and mechanism of photoactivated 5-FU release upon UV-irradiation at lambda(ex)= 365 nm. The photoactivated prodrug 3 derived from conjugation of 2 with a tumor-homing cyclic peptide Cys-Asn-Gly-Arg-Cys (CNGRC) was so designed as to manifest a tumor-targeting function.
MeSH terms
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Anisoles / chemistry
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Antineoplastic Agents / chemical synthesis*
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Drug Delivery Systems
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Ethylamines / chemistry
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Fluorouracil / analogs & derivatives
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Fluorouracil / chemistry*
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Humans
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Lasers
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Molecular Structure
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Peptides, Cyclic / chemistry
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Photochemistry
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Photolysis*
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Prodrugs / chemical synthesis*
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Triazoles / chemistry
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Trimethylsilyl Compounds / chemistry
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Ultraviolet Rays
Substances
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Anisoles
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Antineoplastic Agents
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Ethylamines
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Peptides, Cyclic
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Prodrugs
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Triazoles
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Trimethylsilyl Compounds
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N,N-diisopropylethylamine
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anisole
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Fluorouracil