1. Beta-carbolines as specific inhibitors of cyclin-dependent kinases.
- Author
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Song Y, Wang J, Teng SF, Kesuma D, Deng Y, Duan J, Wang JH, Qi RZ, and Sim MM
- Subjects
- Cyclin-Dependent Kinase 2, Cyclin-Dependent Kinase 5, Cyclin-Dependent Kinase Inhibitor p21, CDC2-CDC28 Kinases, Carbolines pharmacology, Cyclin-Dependent Kinases antagonists & inhibitors, Cyclins pharmacology, Protein Serine-Threonine Kinases antagonists & inhibitors
- Abstract
Harmine (3), 7-fluoro-1-methyl beta-carboline (35) and 1-(5-methyl-imidazol-4-yl) beta-carboline (41) were potent and specific inhibitors of cyclin-dependent kinases. The degree of aromaticity of the tricyclic ring and the positioning of substituents are important for inhibitory activity. While most beta-carbolines inhibited CDK2 and CDK5 to the same extent, selective inhibition against CDK2 was observed in 1-(2-chlorophenyl)- (12), 1-(2-fluorophenyl)- (15), and 1-(2-chloro-5-nitrophenyl)- (28) beta-carbolines.
- Published
- 2002
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