title: Microwave-assisted synthesis and biological evaluation of novel uracil derivatives inhibiting human thymidine phosphorylase.
abstract: New 5-chloro-6-substituted-uracil derivatives have been prepared by microwave assisted-synthesis and tested in vitro as thymidine phosphorylase inhibitors. One of these compounds showed potent inhibitory activity, with an IC50 value in the submicromolar range. The biological activity of the new compounds is discussed in terms of structure-activity relationship.
authors.affiliation: Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Via Aldo Moro, 53100 Siena, Italy. corelli@unisi.it
authors.forename: Federico
authors.initials: F
authors.lastname: Corelli
authors.forename: Maurizio
authors.initials: M
authors.lastname: Botta
authors.forename: Andrea
authors.initials: A
authors.lastname: Lossani
authors.forename: Serena
authors.initials: S
authors.lastname: Pasquini
authors.forename: Silvio
authors.initials: S
authors.lastname: Spadari
authors.forename: Federico
authors.initials: F
authors.lastname: Focher
mesh_terms: D004353:Drug Evaluation, Preclinical / Q000379:methods; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D008872:Microwaves; D013939:Thymidine Phosphorylase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D014498:Uracil / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; D014498:Uracil; D013939:Thymidine Phosphorylase