145208-54-4Relevant academic research and scientific papers
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.
Benzamide nitriles
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Page 34, (2010/02/09)
Compounds of the formula (I) wherein m, n, A, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.
Novel Immunosuppressive Butenamides
Axton, Christopher A.,Billingham, Michael E. J.,Bishop, Paul M.,Gallagher, Peter T.,Hicks, Terence A.,et al.
, p. 2203 - 2214 (2007/10/02)
2-thiophene 12 was carboxylated using butyllithium and carbon dioxide to give 5-thiophene-2-carboxylic acid 13.Conversion of the acid 13 using diphenyl phosphazidate and triethylamine gave 5-4-(1,
