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...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 azaindirubi...展开更多
Twenty 7-azaindirubin derivatives were designed and synthesized. Their antitumor activities were evaluated in vitro against DU145 cell line. The pharmacological results showed that most of the prepared compounds displ...Twenty 7-azaindirubin derivatives were designed and synthesized. Their antitumor activities were evaluated in vitro against DU145 cell line. The pharmacological results showed that most of the prepared compounds displayed the excellent activity. Compound 18 exhibited the most potent antitumor activity among the tested compounds.展开更多
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 azaindirubi...
文摘Twenty 7-azaindirubin derivatives were designed and synthesized. Their antitumor activities were evaluated in vitro against DU145 cell line. The pharmacological results showed that most of the prepared compounds displayed the excellent activity. Compound 18 exhibited the most potent antitumor activity among the tested compounds.
