Literature

Abstract

A series of novel 4-anilinoquinazoline derivatives (3a-3j) has been synthesized and evaluated as potential inhibitors for protein kinases implicated in Alzheimer's disease. Among all the synthesized compounds, compound 3e (N-(3,4-dimethoxyphenyl)-6,7-dimethoxyquinazolin-4-amine) exhibited the most potent inhibitory activity against CLK1 and GSK-3α/β kinase with IC₅₀ values of 1.5 μM and 3 μM, respectively. Docking studies were performed to elucidate the binding mode of the compounds to the active site of CLK1 and GSK-3β. The results of our study suggest that compound 3e may serve as a valuable template for the design and development of dual inhibitors of CLK1 and GSK-3α/β enzymes with potential therapeutic application in Alzheimer's disease.

DOI： 10.1016/j.bmc.2014.01.044

Synthesis, biological evaluation and molecular modelling studies of 4-anilinoquinazoline derivatives as protein kinase inhibitors

Bioorganic & Medicinal Chemistry 2014.0

New pyrido[3,4-g]quinazoline derivatives as CLK1 and DYRK1A inhibitors: synthesis, biological evaluation and binding mode analysis

European Journal of Medicinal Chemistry 2019.0

Discovery of DB18, a potent inhibitor of CLK kinases with a high selectivity against DYRK1A kinase

Bioorganic & Medicinal Chemistry 2021.0

N -(1 H -Pyrazol-3-yl)quinazolin-4-amines as a novel class of casein kinase 1δ/ε inhibitors: Synthesis, biological evaluation and molecular modeling studies

Bioorganic & Medicinal Chemistry Letters 2017.0

Syntheses, neural protective activities, and inhibition of glycogen synthase kinase-3β of substituted quinolines

Bioorganic & Medicinal Chemistry Letters 2014.0

Design, synthesis, evaluation and molecular modeling study of 4-N-phenylaminoquinolines for Alzheimer disease treatment