In vivo targeting of tumor-associated carbonic anhydrases using acetazolamide derivatives
In vivo targeting of tumor-associated carbonic anhydrases using acetazolamide derivatives
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DOI：
10.1016/j.bmcl.2009.06.022
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发表时间：
2009-08-15
影响因子：
2.7
通讯作者：
Neri, Dario
中科院分区：
文献类型：
--
作者：
Ahlskog, Julia K. J.;Dumelin, Christoph E.;Neri, Dario
我们描述了两个含有带电荧光团或白蛋白结合部分的乙酰唑胺衍生物的合成和表征，这两个部分限制了与存在于肿瘤细胞上的碳酸酐酶IX和XII的结合。体内研究表明，在SK-RC-52异种移植癌模型中，荧光乙酰唑胺衍生物优先靶向肿瘤细胞，并具有白蛋白结合的乙酰唑胺衍生物导致肿瘤延迟的能力。(C)2009爱思唯尔有限公司。保留所有权利。
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.