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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 32, Number 3
BKCSDE 32(3)
March 20, 2011 

 
Title
A Blood-brain Barrier Permeable Derivative of 5-Fluorouracil: Preparation, Intracellular Localization, and Mouse Tissue Distribution
Author
Jungkyun Im, Goutam Biswas, Wanil Kim, Kyong Tai Kim, Sung Kee Chung*
Keywords
Blood-brain barrier, G8 molecular transporter, CNS delivery, anti-cancer agent
Abstract
5-Fluorouracil (5-FU), an anticancer agent was covalently attached to the recently developed sorbitol-based G8<BR>transporter, and the conjugate (<STRONG>7</STRONG>) with FITC was found to have an affinity toward mitochondria and to readily<BR>cross BBB to gain an entry into mouse brain. Measured by IC<SUB>50</SUB>, the conjugate (<STRONG>9</STRONG>) without the fluorophore<BR>showed enhanced cytotoxic activity toward two types of multidrug-resistant cell lines. These results strongly<BR>suggest that the sorbitol-based G8 transporter can be utilized as a good CNS delivery vector.
Page
873 - 879
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