857334-83-9Relevant articles and documents
Diarylthiophenes as inhibitors of the pore-forming protein perforin
Miller, Christian K.,Huttunen, Kristiina M.,Denny, William A.,Jaiswal, Jagdish K.,Ciccone, Annette,Browne, Kylie A.,Trapani, Joseph A.,Spicer, Julie A.
, p. 355 - 360 (2016/01/09)
Evolution from a furan-containing high-throughput screen (HTS) hit (1) resulted in isobenzofuran-1(3H)-one (2) as a potent inhibitor of the function of both isolated perforin protein and perforin delivered in situ by intact KHYG-1 NK cells. In the current study, structure-activity relationship (SAR) development towards a novel series of diarylthiophene analogues has continued through the use of substituted-benzene and -pyridyl moieties as bioisosteres for 2-thioxoimidazolidin-4-one (A) on a thiophene (B) -isobenzofuranone (C) scaffold. The resulting compounds were tested for their ability to inhibit perforin lytic activity in vitro. Carboxamide (23) shows a 4-fold increase(2) in lytic activity against isolated perforin and provides good rationale for continued development within this class.
NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
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Page/Page column 21-22, (2010/02/12)
Acetylcholine receptor ligands of formula (I), wherein D, Ar1, E and Ar2 are as described in the specification, diastereoisomers, enantiomers, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for usi
