Photosensitizers related to purpurin-18-N-alkylimides:: A comparative in vivo tumoricidal ability of ester versus amide functionalities

被引：35

作者：

Zheng, G

Potter, WR

Sumlin, A

Dougherty, TJ

Pandey, RK ^{[1
]}

机构：

[1] New York State Dept Hlth, Roswell Pk Canc Inst, Photodynam Therapy Ctr, Buffalo, NY 14263 USA

[2] New York State Dept Hlth, Roswell Pk Canc Inst, Dept Nucl Med, Buffalo, NY 14263 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(99)00649-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 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.

引用

页码：123 / 127

页数：5

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