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ID: ALA1135277

Journal: Bioorg Med Chem Lett

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

Authors: Song Y, Wang J, Teng SF, Kesuma D, Deng Y, Duan J, Wang JH, Qi RZ, Sim MM.

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.

CiteXplore: 11909733

DOI: 10.1016/s0960-894x(02)00094-x