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Bioorg Med Chem Lett. 2002 Apr 8;12(7):1129-32.

Beta-carbolines as specific inhibitors of cyclin-dependent kinases.

Author information

1
Medicinal and Combinatorial Chemistry Group, Institute of Molecular and Cell Biology, 30 Medical Drive, Singapore 117609, Singapore.

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.

PMID:
11909733
DOI:
10.1016/s0960-894x(02)00094-x
[Indexed for MEDLINE]

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