Literature

Abstract

2-Aryl-8-hydroxy (or methoxy)-isoquinolin-1(2H)-one has been proposed as a novel scaffold of EGFR inhibitor based on scaffold hoping. In the present study, a series of 2-aryl-8-hydroxy (or methoxy)-isoquinolin-1(2H)-one derivatives were synthesized. Their antiproliferative activities in vitro were evaluated via MTT assay against two human cancer cell lines, including A431 and A549. The SAR of the title compounds was preliminarily discussed. The compounds with ideal inhibition were evaluated through ELISA-based EGFR-TK assay. Compound 6c showed the best activity against A431 and EGFR tyrosine kinase. These findings suggest that title compounds are EGFR inhibitors with novel structures.

DOI： 10.1016/j.bmc.2013.09.027

Discovery of 2-aryl-8-hydroxy (or methoxy)-isoquinolin-1(2H)-ones as novel EGFR inhibitor by scaffold hopping

Bioorganic & Medicinal Chemistry 2013.0

Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors

Bioorganic & Medicinal Chemistry Letters 2016.0

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

Synthesis and in vitro biological evaluation of novel quinazoline derivatives

Bioorganic & Medicinal Chemistry Letters 2017.0

6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells

European Journal of Medicinal Chemistry 2018.0

Design, synthesis, antiproliferative activity and docking studies of quinazoline derivatives bearing 2,3-dihydro-indole or 1,2,3,4-tetrahydroquinoline as potential EGFR inhibitors