Francis, Stuart published the artcileStructure-based design, synthesis and biological evaluation of a novel series of isoquinolone and pyrazolo[4,3-c]pyridine inhibitors of fascin 1 as potential anti-metastatic agents, Quality Control of 67988-50-5, the main research area is isoquinolone preparation fascin inhibitor antimetastatic agent; pyrazolopyridine preparation fascin inhibitor antimetastatic agent; Cancer; Drug discovery; Fragments; Medicinal chemistry; Virtual screening.
Fascin is an actin binding and bundling protein that is not expressed in normal epithelial tissues but overexpressed in a variety of invasive epithelial tumors. It has a critical role in cancer cell metastasis by promoting cell migration and invasion. Here are reported the crystal structures of fascin in complex with a series of novel and potent inhibitors. Structure-based elaboration of these compounds enabled the development of a series with nanomolar affinities for fascin, good physicochem. properties and the ability to inhibit fascin-mediated bundling of filamentous actin. Compound I (BDP-13176) was found to be the best fascin binder (SPR Kd = 85±0.02 nM, LE=0.29, ITC Kd = 50 nM) and actin bundling inhibitor (IC50 = 240±0.01 nM). These compounds provide promising starting points for fascin-targeted anti-metastatic therapies.
Bioorganic & Medicinal Chemistry Letters published new progress about Actins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 67988-50-5 belongs to class naphthyridine, name is 2,7-Naphthyridin-1(2H)-one, and the molecular formula is C8H6N2O, Quality Control of 67988-50-5.
Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem