Microwave-assisted synthesis and biological evaluation of novel uracil derivatives inhibiting human thymidine phosphorylase

Federico Corelli; Maurizio Botta; Andrea Lossani; Serena Pasquini; Silvio Spadari; Federico Focher

doi:10.1016/j.farmac.2004.08.007

Microwave-assisted synthesis and biological evaluation of novel uracil derivatives inhibiting human thymidine phosphorylase

Farmaco. 2004 Dec;59(12):987-92. doi: 10.1016/j.farmac.2004.08.007.

Authors

Federico Corelli¹, Maurizio Botta, Andrea Lossani, Serena Pasquini, Silvio Spadari, Federico Focher

Affiliation

¹ Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Via Aldo Moro, 53100 Siena, Italy. corelli@unisi.it

PMID: 15598434
DOI: 10.1016/j.farmac.2004.08.007

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Drug Evaluation, Preclinical / methods
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology
Humans
Microwaves*
Thymidine Phosphorylase / antagonists & inhibitors*
Thymidine Phosphorylase / metabolism
Uracil / chemical synthesis*
Uracil / pharmacology

Substances

Enzyme Inhibitors
Uracil
Thymidine Phosphorylase