A Blood-brain Barrier Permeable Derivative of 5-Fluorouracil: Preparation, Intracellular Localization, and Mouse Tissue Distribution

被引：12

作者：

Im, Jungkyun ^{[1
]}

Biswas, Goutam ^{[1
]}

Kim, Wanil ^{[2
]}

Kim, Kyong-Tai ^{[2
]}

Chung, Sung-Kee ^{[1
]}

机构：

[1] Pohang Univ Sci & Technol, Dept Chem, Pohang 790784, South Korea

[2] Pohang Univ Sci & Technol, Dept Life Sci, Pohang 790784, South Korea

来源：

BULLETIN OF THE KOREAN CHEMICAL SOCIETY | 2011年 / 32卷 / 03期

关键词：

Blood-brain barrier; G8 molecular transporter; CNS delivery; anti-cancer agent; CONTAINING MOLECULAR TRANSPORTERS; FLUOROPYRIMIDINE CARBAMATE; CAPECITABINE; MECHANISMS; CANCER; DELIVERY; DESIGN;

D O I：

10.5012/bkcs.2011.32.3.873

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

5-Fluorouracil (5-FU), an anticancer agent was covalently attached to the recently developed sorbitol-based G8 transporter, and the conjugate (7) with FITC was found to have an affinity toward mitochondria and to readily cross BBB to gain an entry into mouse brain. Measured by IC50, the conjugate (9) without the fluorophore showed enhanced cytotoxic activity toward two types of multidrug-resistant cell lines. These results strongly suggest that the sorbitol-based G8 transporter can be utilized as a good CNS delivery vector.

引用

收藏

页码：873 / 879

页数：7

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