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Molecules 2014, 19(9), 13177-13187; doi:10.3390/molecules190913177

Design and Synthesis of New Cholesterol-Conjugated 5-Fluorouracil: A Novel Potential Delivery System for Cancer Treatment

1
Kayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
2
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
*
Author to whom correspondence should be addressed.
Received: 12 May 2014 / Revised: 9 July 2014 / Accepted: 15 July 2014 / Published: 26 August 2014
View Full-Text   |   Download PDF [1981 KB, uploaded 26 August 2014]   |  

Abstract

Cholesterol-conjugated 5-fluorouracil prodrugs were designed to be carried in vivo via low density lipoproteins (LDL) and subsequently undergo LDL-receptor-mediated internalisation into cancer cells. In vivo anti-cancer evaluation was performed using 5-fluorouracil-cholesterol conjugate in a mouse model. The obtained prodrugs were more potent than 5-fluorouracil control drug at the same 5-fluorouracil content (3 mg·kg−1). View Full-Text
Keywords: drug targeting; anticancer; cholesteryl esters drug targeting; anticancer; cholesteryl esters
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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Radwan, A.A.; Alanazi, F.K. Design and Synthesis of New Cholesterol-Conjugated 5-Fluorouracil: A Novel Potential Delivery System for Cancer Treatment. Molecules 2014, 19, 13177-13187.

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