Citation
G. Zheng et al., Photosensitizers related to purpurin-18-N-alkylimides: A comparative in vivo tumoricidal ability of ester versus amide functionalities, BIOORG MED, 10(2), 2000, pp. 123-127
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X
→ ACNP
Volume
10
Issue
2
Year of publication
2000
Pages
123 - 127
Database
ISI
SICI code
0960-894X(20000117)10:2<123:PRTPAC>2.0.ZU;2-Q
Abstract
For a comparative study, 3-(alkyloxyethyl)-3-devinylpurpurin- 18-N-hexylimi
des with ester and amide functionalities were investigated for tumor select
ivity and in vivo photosensitizing efficacy. Compared to amide analogues, t
he related photosensitizers with ester functionalities were found to be mor
e effective. Among these compounds the 3-devinyl-(3-hexyloxyethyl)-purpurin
-18-N-hexylimide as methyl ester 12 showed excellent tumor uptake (tumor ve
rsus muscle ratio: 8:1), and produced 100% tumor cure on day 30 at a dose o
f 1.0 mu mol/kg. The mice were treated with light (135 J/cm(2), 705 nm) at
24 h post injection of the drug. (C) 2000 Elsevier Science Ltd. All rights
reserved.