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Back Cover: Design and Synthesis of Tricyclic JAK3 Inhibitors with Picomolar Affinities as Novel Molecular Probes (ChemMedChem 2/2014)
Author(s) -
Gehringer Matthias,
Pfaffenrot Ellen,
Bauer Silke,
Laufer Stefan A.
Publication year - 2014
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201490004
Subject(s) - tricyclic , chemistry , tofacitinib , affinities , janus kinase 3 , binding affinities , combinatorial chemistry , pharmacology , stereochemistry , receptor , biochemistry , in vitro , medicine , rheumatoid arthritis , cytotoxic t cell , antigen presenting cell
The back cover picture shows the design of a novel class of tricyclic Janus kinase 3 (JAK3) inhibitors. By freezing the current gold standard, tofacitinib, into its binding conformation, extremely potent inhibitors with improved selectivity for JAK3 and intracellular activity were developed. These compounds may serve as tools and probes for pharmacodynamic studies. For more details, see the Communication by Stefan A. Laufer et al. on p. 277 ff.