Literature

Abstract

A series of novel quinazoline derivatives bearing various C-6 benzamide substituents were synthesized and evaluated as EGFR inhibitors, and most showed significant inhibitory potency against EGFR kinase. In particular, compound 6g possessed potent inhibitory activity against EGFR wild-type (IC = 5 nM), and strong antiproliferative activity against HCC827 and Ba/F3 (L858R) cell lines. Kinase profiling against a panel of 365 kinases showed that 6g was highly selective for EGFR. Furthermore, 6g showed desirable properties in assays of liver microsome metabolic stability and cytochromes P450 inhibition and preliminary pharmacokinetic study. The overall attractive profile of 6g made it an interesting compound for further development.

DOI： 10.1016/j.bmc.2018.02.022

Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors

Bioorganic & Medicinal Chemistry 2018.0

Novel 4-arylaminoquinazoline derivatives with ( E )-propen-1-yl moiety as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells

European Journal of Medicinal Chemistry 2017.0

Facile and efficient synthesis and biological evaluation of 4-anilinoquinazoline derivatives as EGFR inhibitors

Bioorganic & Medicinal Chemistry Letters 2016.0

Synthesis and in vitro biological evaluation of novel quinazoline derivatives

Bioorganic & Medicinal Chemistry Letters 2017.0

Four-membered heterocycles-containing 4-anilino-quinazoline derivatives as epidermal growth factor receptor (EGFR) kinase inhibitors

Bioorganic & Medicinal Chemistry Letters 2013.0

Design, synthesis and in vitro anti-proliferative activity of 4,6-quinazolinediamines as potent EGFR-TK inhibitors