Design, Synthesis, and Evaluation of Indolinones as Inhibitors of the Transforming Growth Factor β Receptor I (TGFβRI)

Inhibition of transforming growth factor β (TGFβ) type I receptor (Alk5) offers a novel approach for the treatment of fibrotic diseases and cancer. Indolinones substituted in position 6 were identified as a new chemotype inhibiting TGFβRI concomitant with a low cross-reactivity among the human kinom...

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Veröffentlicht in:	Journal of medicinal chemistry 2010-10, Vol.53 (20), p.7287-7295
Hauptverfasser:	Roth, Gerald J, Heckel, Armin, Brandl, Trixi, Grauert, Matthias, Hoerer, Stefan, Kley, Joerg T, Schnapp, Gisela, Baum, Patrick, Mennerich, Detlev, Schnapp, Andreas, Park, John E
Format:	Artikel
Sprache:	eng
Schlagworte:	Cell Line Crystallography, X-Ray Drug Design Humans Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Models, Molecular Phosphorylation Protein-Serine-Threonine Kinases - antagonists & inhibitors Protein-Serine-Threonine Kinases - chemistry Receptor, Platelet-Derived Growth Factor alpha - antagonists & inhibitors Receptors, Transforming Growth Factor beta - antagonists & inhibitors Receptors, Transforming Growth Factor beta - chemistry Smad2 Protein - metabolism Smad3 Protein - metabolism Stereoisomerism Structure-Activity Relationship
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