In vivo targeting of tumor-associated carbonic anhydrases using acetazolamide derivatives

被引：147

作者：

Ahlskog, Julia K. J. ^{[1
]}

Dumelin, Christoph E. ^{[2
]}

Truessel, Sabrina ^{[1
]}

Marlind, Jessica ^{[1
]}

Neri, Dario ^{[1
]}

机构：

[1] ETH, Inst Pharmaceut Sci, Dept Chem & Appl Biosci, CH-8093 Zurich, Switzerland

[2] ETH, Philochem AG, CH-8093 Zurich, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 16期

基金：

瑞士国家科学基金会;

关键词：

Carbonic anhydrase; CA IX; CA XII; Acetazolamide; Tumor targeting; RENAL-CELL CARCINOMA; PRE-MESSENGER-RNA; MONOCLONAL-ANTIBODY; EXTRACELLULAR PH; ALBUMIN-BINDING; CANCER-THERAPY; TENASCIN-C; HYPOXIA; IX; INHIBITORS;

D O I：

10.1016/j.bmcl.2009.06.022

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We describe the synthesis and characterization of two acetazolamide derivatives containing either a charged fluorophore or an albumin-binding moiety, which restrict binding to carbonic anhydrase IX and XII present on tumor cells. In vivo studies showed the preferentially targeting of tumor cells by the fluorescent acetazolamide derivative and the ability of the albumin-binding acetazolamide derivative to cause tumor retardation in a SK-RC-52 xenograft model of cancer. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4851 / 4856

页数：6

共 37 条

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