Synthesis and CDK2 kinase inhibitory activity of 7/7′-azaindirubin derivatives |
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Authors: | Zhao Hui Wang Ying Dong Tao Wang Ming Hong Shang Wei Yi Hua Qi Zheng Yao |
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Institution: | a Department of Organic Chemistry, China Pharmaceutical University, Nanjing 210009, China;b Jiangsu Center for Drug Screening, China Pharmaceutical University, Nanjing 210009, China;c School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China |
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Abstract: | 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. |
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Keywords: | 7'-Azaindirubin 7-Azaindirubin Synthesis CDK2/cyclinA Inhibition |
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