title: Design and synthesis of new cholesterol-conjugated 5-Fluorouracil: a novel potential delivery system for cancer treatment.
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).
authors.affiliation: Kayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. dhna_2001@hotmail.com.
authors.forename: Awwad A
authors.initials: AA
authors.lastname: Radwan
authors.affiliation: Kayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. afars04@yahoo.com.
authors.forename: Fares K
authors.initials: FK
authors.lastname: Alanazi
mesh_terms: D000818:Animals; D002784:Cholesterol / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000737:chemistry; D016503:Drug Delivery Systems; D015195:Drug Design; D005472:Fluorouracil / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000737:chemistry; D006801:Humans; D008077:Lipoproteins, LDL / Q000737:chemistry / Q000378:metabolism; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy*; D011973:Receptors, LDL / Q000737:chemistry / Q000378:metabolism
chemical_list: D008077:Lipoproteins, LDL; D011973:Receptors, LDL; D002784:Cholesterol; D005472:Fluorouracil