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.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Amination
-
Animals
-
Antineoplastic Agents / chemical synthesis
-
Antineoplastic Agents / chemistry
-
Antineoplastic Agents / therapeutic use
-
Catalysis
-
Cell Line, Tumor
-
Chlorine / chemistry*
-
Glycogen Synthase Kinase 3 / metabolism
-
Glycogen Synthase Kinase 3 beta
-
Humans
-
Indazoles / chemical synthesis
-
Indazoles / chemistry*
-
Indazoles / pharmacology*
-
Mice
-
Mice, Nude
-
Molecular Structure
-
Neoplasms / drug therapy
-
Neoplasms / pathology
-
Phosphorylation / drug effects
-
Protein Kinase Inhibitors / chemical synthesis*
-
Protein Kinase Inhibitors / chemistry
-
Protein Kinase Inhibitors / pharmacology*
-
Proto-Oncogene Proteins c-akt / antagonists & inhibitors*
-
Proto-Oncogene Proteins c-akt / metabolism
-
Structure-Activity Relationship
-
Xenograft Model Antitumor Assays
Substances
-
Antineoplastic Agents
-
Indazoles
-
Protein Kinase Inhibitors
-
Chlorine
-
Glycogen Synthase Kinase 3 beta
-
Proto-Oncogene Proteins c-akt
-
Glycogen Synthase Kinase 3