Mechanistic Study of Potent Fluorinated EGFR Kinase Inhibitors with a Quinazoline Scaffold against L858R/T790M/C797S Resistance Mutation: Unveiling the Fluorine Substituent Cooperativity Effect on the Inhibitory Activity.

Farideh Badichi Akher,Abdolkarim Farrokhzadeh,Neil Ravenscroft,Michelle M. Kuttel

Mechanistic Study of Potent Fluorinated EGFR Kinase Inhibitors with a Quinazoline Scaffold against L858R/T790M/C797S Resistance Mutation: Unveiling the Fluorine Substituent Cooperativity Effect on the Inhibitory Activity.

2020

Farideh Badichi Akher
Abdolkarim Farrokhzadeh
Neil Ravenscroft
Michelle M. Kuttel

Fluorination has considerable potential with regard to the design of kinase inhibitors for anticarcinoma therapy. It was recently reported that fluorination increases the potency of inhibitors of t...

Keywords:

Kinase
Potency
T790M
Epidermal growth factor receptor
Cooperativity
Resistance mutation
Photochemistry
Stereochemistry
Chemistry
Quinazoline
Substituent

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