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We present the design, synthesis and biological activity of a new series of substituted 3-(2-(1H-indol-1-yl)ethyl)-1H-indoles and 1,2-di(1H-indol-1-yl)alkanes as selective inhibitors of CDK4/cyclin D1. The compounds were designed to explore the relationship between the connection mode of the indolyl moieties and their CDK inhibitory activities. We found all the above-mentioned designed compounds to be selective inhibitors of CDK4/cyclin D1 compared to the closely related CDK2/cyclin A, with IC(50) for the best compounds 10m and 13a being 39 and 37microm, respectively.

Original publication




Journal article


Bioorg Med Chem

Publication Date





6073 - 6084


Binding Sites, Computer Simulation, Cyclin A, Cyclin D1, Cyclin-Dependent Kinase 2, Cyclin-Dependent Kinase 4, Drug Design, Humans, Indoles, Protein Kinase Inhibitors