Identification of novel inhibitors of UDP-Glc 4???-epimerase, a validated drug target for african sleeping sickness

Urbaniak MD, Tabudravu JN, Msaki A, Matera KM, Brenk R, Jaspars M, Ferguson MAJ
Bioorganic and Medicinal Chemistry Letters - vol. 16 5744-5747 (2006)

Bioorganic and Medicinal Chemistry Letters

Novel inhibitors of Trypanosoma brucei and mammalian UDP-Glc 4???-epimerase were identified by screening a small library of natural products and commercially available drug-like molecules. The inhibitors possess low micromolar potency against the T. brucei and human enzymes in vitro, display a degree of selectivity between the two enzymes, and are cytotoxic to cultured T. brucei and mammalian cells. ?? 2006 Elsevier Ltd. All rights reserved.