Citation: Zhao Hui Wang, Ying Dong, Tao Wang, Ming Hong Shang, Wei Yi Hua, Qi Zheng Yao. Synthesis and CDK2 kinase inhibitory activity of 7/7'-zaindirubin derivatives[J]. Chinese Chemical Letters, ;2010, 21(3): 297-300. doi: 10.1016/j.cclet.2009.11.029 shu

Synthesis and CDK2 kinase inhibitory activity of 7/7'-zaindirubin derivatives

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

Received Date: 14 July 2009

A series of novel 7'-azaindiruubin (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 azaindimbins 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.
- 7'-Azaindirubin,
- 7-Azaindirubin,
- Synthesis,
- CDK2/cyclinA,
- Inhibition
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