Document Report Card
Basic Information
ID: ALA3779893
Journal: Bioorg Med Chem Lett
Title: Identification of novel GLUT inhibitors.
Authors: Siebeneicher H, Bauser M, Buchmann B, Heisler I, Müller T, Neuhaus R, Rehwinkel H, Telser J, Zorn L.
Abstract: The compound class of 1H-pyrazolo[3,4-d]pyrimidines was identified using HTS as very potent inhibitors of facilitated glucose transporter 1 (GLUT1). Extensive structure-activity relationship studies (SAR) of each ring system of the molecular framework was established revealing essential structural motives (i.e., ortho-methoxy substituted benzene, piperazine and pyrimidine). The selectivity against GLUT2 was excellent and initial in vitro and in vivo pharmacokinetic (PK) studies are encouraging.
CiteXplore: 26949183