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

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

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 $IC_{50}$, the conjuga...

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Veröffentlicht in:Bulletin of the Korean Chemical Society 2011, Vol.32 (3), p.873-879
Hauptverfasser: Im, Jung-Kyun, Biswas, Goutam, Kim, Wan-Il, Kim, Kyong-Tai, Chung, Sung-Kee
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container_issue 3
container_start_page 873
container_title Bulletin of the Korean Chemical Society
container_volume 32
creator Im, Jung-Kyun
Biswas, Goutam
Kim, Wan-Il
Kim, Kyong-Tai
Chung, Sung-Kee
description 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 $IC_{50}$, 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.
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title A Blood-brain Barrier Permeable Derivative of 5-Fluorouracil: Preparation, Intracellular Localization, and Mouse Tissue Distribution
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