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Traceless Solid‐Phase Synthesis of 2‐Aminothiazoles: Receptor Tyrosine Kinase Inhibitors with Dual Selectivity for Tie‐2 and VEGFR‐2
Author(s) -
Stieber Frank,
Mazitschek Ralph,
Soric Natascha,
Giannis Athanassios,
Waldmann Herbert
Publication year - 2002
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200290040
Subject(s) - chemistry , receptor tyrosine kinase , tyrosine kinase , selectivity , linker , combinatorial chemistry , ror1 , kinase insert domain receptor , kinase , receptor , vegf receptors , platelet derived growth factor receptor , cancer research , vascular endothelial growth factor , biochemistry , vascular endothelial growth factor a , biology , computer science , growth factor , operating system , catalysis
A 10‐step (!) solid‐phase synthesis employing the traceless hydrazide linker provides efficient access to a 2‐aminothiazole library (see scheme) that yielded access to a new class of tyrosine kinase inhibitors with dual selectivity for the vascular endothelial growth factor receptor VEGFR‐2 and the Tie‐2 receptor tyrosine kinases.