Design and Synthesis of Tetrahydropyridothieno[2,3-d]pyrimidine Scaffold Based Epidermal Growth Factor Receptor (EGFR) Kinase Inhibitors: The Role of Side Chain Chirality and Michael Acceptor Group for Maximal Potency

2010 ◽  
Vol 53 (20) ◽  
pp. 7316-7326 ◽  
Author(s):  
Chia-Hsien Wu ◽  
Mohane Selvaraj Coumar ◽  
Chang-Ying Chu ◽  
Wen-Hsing Lin ◽  
Yi-Rong Chen ◽  
...  
Keyword(s):  
Epidermal Growth Factor Receptor ◽  
Kinase Inhibitors ◽  
Growth Factor Receptor ◽  
Side Chain ◽  
Design And Synthesis ◽  
Acceptor Group ◽  
Michael Acceptor ◽  
Epidermal Growth ◽  
Egfr Kinase

scholarly journals Platination of cysteine by an epidermal growth factor receptor kinase-targeted hybrid agent

2018 ◽  
Vol 54 (54) ◽  
pp. 7479-7482 ◽  
Author(s):  
Mu Yang ◽  
Hanzhi Wu ◽  
Julie Chu ◽  
Lucas A. Gabriel ◽  
Y. Kim ◽  
...  
Keyword(s):  
Epidermal Growth Factor Receptor ◽  
Growth Factor ◽  
Epidermal Growth Factor ◽  
Kinase Inhibitors ◽  
Growth Factor Receptor ◽  
Cysteine Residue ◽  
Receptor Kinase ◽  
Epidermal Growth ◽  
Hybrid Agent ◽  
Egfr Kinase

Platinum-modified tyrosine kinase inhibitors show strong and selective EGFR kinase binding and form adducts with a pharmacologically relevant cysteine residue.

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