Diarylthiophenes as inhibitors of the pore-forming protein perforin
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Graphical abstract
Abbreviations
HTS
high-throughput screen
SAR
structure–activity relationships
PRF
perforin
CTL
cytotoxic T lymphocytes
NK
natural killer cells
PAINS
pan-assay interference compounds
AgNO3
silver(I) nitrate
KF
potassium fluoride
PFP
pentafluorophenyl
DCC
N,N′-dicyclohexylcarbodiimide
HOBt
hydroxybenzotriazole
EDCI
1-ethyl-3-(3-dimethylaminopropyl)carbodiimide
DMF
dimethylformamide
KOAc
potassium acetate
DMSO
dimethyl sulfoxide
THF
tetrahydrofuran
Keywords
Perforin
Perforin inhibitor
Diarylthiophene
Bioisostere
Immunosuppressant
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Copyright © 2015 The Authors. Published by Elsevier Ltd.