Current time in Korea 15:29 Oct 21 (Sat) Year 2017 KCS KCS Publications
KCS Publications
My Journal Log In Register
HOME > Search > Browsing(BKCS) > Archives

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 

A Blood-brain Barrier Permeable Derivative of 5-Fluorouracil: Preparation, Intracellular Localization, and Mouse Tissue Distribution
Jungkyun Im, Goutam Biswas, Wanil Kim, Kyong Tai Kim, Sung Kee Chung*
Blood-brain barrier, G8 molecular transporter, CNS delivery, anti-cancer agent
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.
873 - 879
Full Text