Synthesis and biological evaluation of 5-arylamino-6-chloro-1H-indazole-4, 7-diones as inhibitors of protein kinase B/Akt

…, SW Yeon, JS Ryu, TY Kim, EH Song, HJ You…

Index: Ko, Jong Hee; Yeon, Seung Woo; Ryu, Jung Su; Kim, Tae-Yong; Song, Eun-Ha; You, Hea-Jung; Park, Rae-Eun; Ryu, Chung-Kyu Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 23 p. 6001 - 6005

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Citation Number: 27

Abstract

A series of 5-arylamino-6-chloro-1H-indazole-4, 7-diones were synthesized and evaluated for their inhibitory activity on protein kinase B/Akt. The compounds exhibited a potent Akt1 inhibitory activity. Further mechanistic study revealed that they might have dual inhibitory effects on both activity and phosphorylation of Akt1 in PC-3 tumor cell line.