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Beta-carbolines as specific inhibitors of cyclin-dependent kinases.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2002 Apr 08; Vol. 12 (7), pp. 1129-32. - Publication Year :
- 2002
-
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.
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 12
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 11909733
- Full Text :
- https://doi.org/10.1016/s0960-894x(02)00094-x