Synthesis and CDK2 kinase inhibitory activity of 7/7′-azaindirubin derivatives

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• 作者：Zhao Hui Wang ; Ying Dong ; Tao Wang ; Ming Hong Shang ; Wei Yi Hua ; Qi Zheng Yao
• 关键词：7′ ; -Azaindirubin ; 7-Azaindirubin ; Synthesis ; CDK2/cyclinA ; Inhibition
• 刊名：Chinese Chemical Letters
• 出版年：2010
• 出版时间：March 2010
• 年：2010
• 卷：21
• 期：3
• 页码：297-300
• 全文大小：163 K

文摘

A series of novel 7′-azaindirubin (1a–g) and 7-azaindirubin (2a, 2c, 2e and 2f) derivatives were designed and synthesized. Their structures were characterized by ¹H NMR and MS spectroscopy as well as by elemental analysis. Their inhibitory properties against CDK2/cylinA were evaluated in vitro. In contrast to indirubin, some of the described azaindirubins emerged as potent inhibitors of CDK2/cylinA and compound 2b had more potent activity. Biological tests also showed that nitrogen atom at 7-position of azaindirubin was more beneficial to enhance the kinase inhibitory activity.