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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

Kayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
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]   |  


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

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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