198823-31-3Relevant articles and documents
Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor Activation
Venukadasula, Phanindra K. M.,Owusu, Benjamin Y.,Bansal, Namita,Ross, Larry J.,Hobrath, Judith V.,Bao, Donghui,Truss, Jackie W.,Stackhouse, Murray,Messick, Troy E.,Klampfer, Lidija,Galemmo, Robert A.
, p. 177 - 181 (2016)
In this letter we report first nonpeptide inhibitors of hepatocyte growth factor (HGF) activation. These compounds inhibit the three proteases (matriptase, hepsin, and HGF activator) required for HGF maturation. We show that 6, 8a, 8b, and 8d block activation of fibroblast-derived pro-HGF, thus preventing fibroblast-induced scattering of DU145 prostate cancer cells. Compound 6 (SRI 31215) is very soluble (91 μM) and has excellent microsome stability (human t1/2 = 162 min; mouse t1/2 = 296 min). In mouse 6 has an in vivo t1/2 = 5.8 h following IV administration. The high solubility of 6 and IV t1/2 make this compound a suitable prototype "triplex inhibitor" for the study of the inhibition of HGF activation in vivo.
N-(AMIDINOPHENYL) CYCLOUREA ANALOGS AS FACTOR XA INHIBITORS
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, (2008/06/13)
The present application describes N-(amidinophenyl)cyclourea analogs of formula I: STR1 which are useful as inhibitors of factor Xa.
