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

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...

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Main Authors: Awwad A. Radwan, Fares K. Alanazi
Format: Article
Language:English
Published: MDPI AG 2014-08-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/19/9/13177
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spelling doaj-52c1b38010c24b3cb3da1eec2654535f2020-11-24T23:31:05ZengMDPI AGMolecules1420-30492014-08-01199131771318710.3390/molecules190913177molecules190913177Design and Synthesis of New Cholesterol-Conjugated 5-Fluorouracil: A Novel Potential Delivery System for Cancer TreatmentAwwad A. Radwan0Fares K. Alanazi1Kayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaKayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaCholesterol-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).http://www.mdpi.com/1420-3049/19/9/13177drug targetinganticancercholesteryl esters
collection DOAJ
language English
format Article
sources DOAJ
author Awwad A. Radwan
Fares K. Alanazi
spellingShingle Awwad A. Radwan
Fares K. Alanazi
Design and Synthesis of New Cholesterol-Conjugated 5-Fluorouracil: A Novel Potential Delivery System for Cancer Treatment
Molecules
drug targeting
anticancer
cholesteryl esters
author_facet Awwad A. Radwan
Fares K. Alanazi
author_sort Awwad A. Radwan
title Design and Synthesis of New Cholesterol-Conjugated 5-Fluorouracil: A Novel Potential Delivery System for Cancer Treatment
title_short Design and Synthesis of New Cholesterol-Conjugated 5-Fluorouracil: A Novel Potential Delivery System for Cancer Treatment
title_full Design and Synthesis of New Cholesterol-Conjugated 5-Fluorouracil: A Novel Potential Delivery System for Cancer Treatment
title_fullStr Design and Synthesis of New Cholesterol-Conjugated 5-Fluorouracil: A Novel Potential Delivery System for Cancer Treatment
title_full_unstemmed Design and Synthesis of New Cholesterol-Conjugated 5-Fluorouracil: A Novel Potential Delivery System for Cancer Treatment
title_sort design and synthesis of new cholesterol-conjugated 5-fluorouracil: a novel potential delivery system for cancer treatment
publisher MDPI AG
series Molecules
issn 1420-3049
publishDate 2014-08-01
description 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).
topic drug targeting
anticancer
cholesteryl esters
url http://www.mdpi.com/1420-3049/19/9/13177
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