title: Chemical and biological degradation of 5-fluorouracil prodrugs having high serum albumin binding potencies.
abstract: In order to understand the fundamental structural features which yield both high serum albumin binding potency and desired property as a prodrug, the derivatization was performed at N-1 or N-3 position in 5-fluorouracil. The N-3 derivatives were more stable than N-1 derivatives in vitro, whereas they were metabolized quickly in vivo. It is suggested that N-1 position should be blocked to avoid fast metabolism in vivo.
authors.affiliation: Department of Chemistry, Faculty of Science, Osaka University, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Suda
authors.forename: K
authors.initials: K
authors.lastname: Shimidzu
authors.forename: M
authors.initials: M
authors.lastname: Sumi
authors.forename: S
authors.initials: S
authors.lastname: Kusumoto
authors.forename: T
authors.initials: T
authors.lastname: Nadai
authors.forename: S
authors.initials: S
authors.lastname: Yamashita
mesh_terms: D000818:Animals; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D005472:Fluorouracil / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000493:pharmacokinetics*; D011355:Prodrugs / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D011485:Protein Binding; D051381:Rats; D012709:Serum Albumin / Q000378:metabolism
chemical_list: D011355:Prodrugs; D012709:Serum Albumin; D005472:Fluorouracil