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Photosensitizers related to purpurin-18- N -alkylimides: a comparative in vivo tumoricidal ability of ester versus amide functionalities
January 2000
January 2000
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Abstract
For a comparative study, 3-(alkyloxyethyl)-3-devinylpurpurin-18-N-hexylimides with
ester and amide functionalities were investigated for tumor selectivity and in vivo
photosensitizing efficacy. Compared to amide analogues, the related photosensitizers
with ester functionalities were found to be more effective. Among these compounds
the 3-devinyl-(3-hexyloxyethyl)-purpurin-18-N-hexylimide as methyl ester 12 showed
excellent tumor uptake (tumor versus muscle ratio: 8:1), and produced 100% tumor cure
on day 30 at a dose of 1.0 micromol/kg. The mice were treated with light (135 J/cm2,
705 nm) at 24 h post injection of the drug.