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

Autor:	Wei Yi Hua, Qi Zheng Yao, Ying Dong, Tao Wang, Zhao-Hui Wang, Ming Hong Shang
Rok vydání:	2010
Předmět:	biology Kinase Stereochemistry Cyclin-dependent kinase 2 General Chemistry Inhibitory postsynaptic potential Combinatorial chemistry In vitro chemistry.chemical_compound chemistry Nitrogen atom biology.protein Proton NMR Indirubin
Zdroj:	Chinese Chemical Letters. 21:297-300
ISSN:	1001-8417
DOI:	10.1016/j.cclet.2009.11.029
Popis:	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 1 H 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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::a68a1fb1bd64bf66dca990afa4b44ff2 https://doi.org/10.1016/j.cclet.2009.11.029 Zobrazit plný text záznamu Full Text from ScienceDirect