Synthesis and preliminary in vitro kinase inhibition evaluation of new diversely substituted pyrido[3,4-g]quinazoline derivatives

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• 作者：Wael Zeinyeh^a ; ^b ; Yannick J. Esvan^a ; ^b ; Lionel Nauton^a ; ^b ; Nadè ; ge Loaë ; c^c ; Laurent Meijer^c ; Vincent Thé ; ry^a ; ^b ; Fabrice Anizon^a ; ^b ; Francis Giraud^a ; ^b ; ^{Francis.GIRAUD@univ-bpclermont.fr" class="auth_mail" title="E-mail the corresponding author} ; Pascale Moreau^a ; ^b ; ^{Pascale.MOREAU@univ-bpclermont.fr" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Pyrido[3 ; 4-g]quinazoline ; Protein kinase inhibition ; CLK1 ; DYRK1A ; CDK5 ; GSK3 ; CK1
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 September 2016
• 年：2016
• 卷：26
• 期：17
• 页码：4327-4329
• 全文大小：620 K

文摘

The synthesis of new diversely substituted pyrido[3,4-g]quinazolines is described. The inhibitory potencies of prepared compounds toward a panel of five CMGC protein kinases (CDK5, CLK1, DYRK1A, CK1, GSK3), that are known to play a potential role in Alzheimer’s disease, were evaluated. The best overall kinase inhibition profile was found for nitro compound 4 bearing an ethyl group at the 5-position.