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  • Synthesis and photochemical properties of photoactivated antitumor prodrugs releasing 5-fluorouracil.

Synthesis and photochemical properties of photoactivated antitumor prodrugs releasing 5-fluorouracil.

Organic & biomolecular chemistry (2005-02-11)
Zhouen Zhang, Hiroshi Hatta, Takeo Ito, Sei-ichi Nishimoto
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
N-Ethyldiisopropylamine solution, suitable for peptide synthesis, ~2 M in 1-methyl-2-pyrrolidinone
Sigma-Aldrich
N-Ethyldiisopropylamine, BASF quality, ≥98.0%
Sigma-Aldrich
N,N-Diisopropylethylamine, purified by redistillation, 99.5%
Sigma-Aldrich
N,N-Diisopropylethylamine, ReagentPlus®, ≥99%
Sigma-Aldrich
N,N-Diisopropylethylamine, 99.5%, biotech. grade