544451-83-4Relevant academic research and scientific papers
SUBSTITUTED PYRAZOLOPYRIMIDINES USEFUL AS KINASES INHIBITORS
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Paragraph 00102; 00103; 00104, (2019/02/25)
Disclosed are novel pyrzaolopyrimidines of Formula (I), their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds have protein kinases inhibitory activities and are expected to be useful for the treatment of protei
Solid-phase parallel synthesis and SAR of 4-amidofuran-3-one inhibitors of cathepsin S: Effect of sulfonamides P3 substituents on potency and selectivity
Ayesa, Susana,Lindquist, Charlotta,Agback, Tatiana,Benkestock, Kurt,Classon, Bjoern,Henderson, Ian,Hewitt, Ellen,Jansson, Katarina,Kallin, Anders,Sheppard, Dave,Samuelsson, Bertil
experimental part, p. 1307 - 1324 (2009/08/08)
Highly potent and selective 4-amidofuran-3-one inhibitors of cathepsin S are described. The synthesis and structure-activity relationship of a series of inhibitors with a sulfonamide moiety in the P3 position is presented. Several members of the series show sub-nanomolar inhibition of the target enzyme as well as an excellent selectivity profile and good cellular potency. Molecular modeling of the most interesting inhibitors describes interactions in the extended S3 pocket and explains the observed selectivity towards cathepsin K.
