Literature

Abstract

Quinazoline-containing derivatives are an important class of synthetic products and represent an attractive scaffold for EGFR inhibitors. A series of oxazolo[4,5-g]quinazolin-2(1H)-one derivatives were synthesized and the EGFR and Src inhibition activities were evaluated using Gefitinib as lead compound. The three most potent compounds 5y, 5l and 5a each inhibited EGFR at the IC(50) value of 61 nM, 67 nM and 78 nM. Among them, 5c also demonstrated excellent inhibition activity against Src with the IC(50) value of 3.1 μM. Several of these derivatives also showed good anti-proliferation effects against KB and A498 cells.

DOI： 10.1016/j.ejmech.2012.06.055

Novel oxazolo[4,5-g]quinazolin-2(1H)-ones: Dual inhibitors of EGFR and Src protein tyrosine kinases

European Journal of Medicinal Chemistry 2012.0

Design, synthesis and biological evaluation of novel 3,4-dihydro-2H-[1,4]oxazino [2,3-f]quinazolin derivatives as EGFR-TKIs

Bioorganic & Medicinal Chemistry Letters 2023.0

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

Bioorganic & Medicinal Chemistry Letters 2016.0

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

Bioorganic & Medicinal Chemistry Letters 2016.0

Synthesis and in vitro biological evaluation of novel quinazoline derivatives

Bioorganic & Medicinal Chemistry Letters 2017.0

Design, synthesis, anti-tumor activity, and molecular modeling of quinazoline and pyrido[2,3-d]pyrimidine derivatives targeting epidermal growth factor receptor