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

TY - JOUR

T1 - Identification of novel inhibitors of UDP-Glc 4 '-epimerase, a validated drug target for African sleeping sickness

AU - Urbaniak, Michael D.

AU - Tabudravu, Jioji N.

AU - Msaki, Aichi

AU - Matera, Kathy Mansfield

AU - Brenk, Ruth

AU - Jaspars, Marcel

AU - Ferguson, Michael A. J.

PY - 2006/11/15

Y1 - 2006/11/15

N2 - 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. (c) 2006 Elsevier Ltd. All rights reserved.

AB - 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. (c) 2006 Elsevier Ltd. All rights reserved.

U2 - 10.1016/j.bmcl.2006.08.091

DO - 10.1016/j.bmcl.2006.08.091

M3 - Article

SN - 0960-894X

VL - 16

SP - 5744

EP - 5747

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 22

ER -