540523-98-6Relevant articles and documents
Synthesis and in vitro characterization of novel fluorinated derivatives of the TSPO 18 kDa ligand SSR180575
Damont, Annelaure,Marguet, Frank,Puech, Frédéric,Dollé, Frédéric
, p. 736 - 745 (2015/08/04)
Abstract SSR180575 (1) is a high-affinity (0.83 nM) TSPO 18 kDa ligand belonging to the pyridazino[4,5-b]indole-1-acetamides family. Herein we describe the synthesis and in vitro characterization of two series of new fluorinated analogues. Eleven compounds (out of fifteen) displayed nanomolar to subnamolar affinities (0.30-8.1 nM) and high selectivities (Ki(CBR)/Ki(TSPO) > 103). Two derivatives stand out as promising candidates for drug development or use as PET probes for in vivo neuroinflammation imaging, once fluorine-18-labelled.
NOVEL P53-MDM2/P53-MDM4 ANTAGONISTS TO TREAT PROLIFERATIVE DISEASE
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Page/Page column 16, (2011/09/30)
High-resolution structural information delineates key interactions between MDM2 or MDM4 and heterocyclic compounds that bind to these proteins. These compounds are potent agonists of the p53-MDM2/p53-MDM4 complex.
Methods for the use of inhibitors of cytosolic phospholipase A2 in the treatment of thrombosis
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Page/Page column 30, (2010/11/29)
This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds in the treating or preventing thrombosis in a mammal, or preventing progression of symptoms of thrombosis.