Kinase inhibitions in pyrido[4,3-h] and [3,4-g]quinazolines: Synthesis, SAR and molecular modeling studies

被引：10

作者：

Zeinyeh, Wael ^{[1
]}

Esvan, Yannick J. ^{[1
]}

Josselin, Beatrice ^{[2
]}

Baratte, Blandine ^{[2
]}

Bach, Stephane ^{[2
]}

Nauton, Lionel ^{[1
]}

Thery, Vincent ^{[1
]}

Ruchaud, Sandrine ^{[2
]}

Anizon, Fabrice ^{[1
]}

Giraud, Francis ^{[1
]}

Moreau, Pascale ^{[1
]}

机构：

[1] Univ Clermont Auvergne, CNRS, SIGMA Clermont, ICCF, F-63000 Clermont Ferrand, France

[2] Sorbonne Univ, Plateforme Criblage KISSf Kinase Inhibitor Specia, Prot Phosphorylat & Human Dis Unit, CNRS,Stn Biol, Pl Georges Teissier, F-29688 Roscoff, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2019年 / 27卷 / 10期

关键词：

Pyrido[3,4-g]quinazolines; Pyrido[4,3-h]quinazoline; Protein kinase inhibition; CLK1; CLK1; DERIVATIVES; DYRK1A;

D O I：

10.1016/j.bmc.2019.04.005

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

New pyrido[3,4-g]quinazoline derivatives were prepared and evaluated for their inhibitory potency toward 5 protein kinases (CLK1, DYRK1A, GSK3, CDK5, CK1). A related pyrido[4,3-h]quinazoline scaffold with an angular structure was also synthesized and its potency against the same protein kinase panel was compared to the analogous pyrido[3,4-g] quinazoline. Best results were obtained for 10-nitropyrido[3,4-g]quinazoline 4 toward CLK1 with nanomolar activities.

引用

页码：2083 / 2089

页数：7

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