175293-38-6Relevant articles and documents
Hydrazinonaphthalene and azonaphthalene thrombopoietin mimics are nonpeptidyl promoters of megakaryocytopoiesis
Duffy,Darcy,Delorme,Dillon,Eppley,Erickson-Miller,Giampa,Hopson,Huang,Keenan,Lamb,Leong,Liu,Miller,Price,Rosen,Shah,Shaw,Smith,Stark,Tian,Tyree,Wiggall,Zhang,Luengo
, p. 3730 - 3745 (2007/10/03)
High-throughput screening for the induction of a luciferase reporter gene in a thrombopoietin (TPO)-responsive cell line resulted in the identification of 4-diazo-3-hydroxy-1-naphthalene-sulfonic acids as TPO mimics. Modification of the core structure and adjustment of unwanted functionality resulted in the development of (5-oxo-1,5-dihydropyrazol-4-ylidene)hydrazines which exhibited efficacies equivalent to those of TPO in several cell-based assays designed to measure thrombopoietic activity. Furthermore, these compounds elicited biochemical responses in TPO-receptor-expressing cells similar to those in TPO itself, including kinase activation and protein phosphorylation. Potencies for the best compounds were high for such low molecular weight compounds (MW 50 values in the region of 1-20 nM.
