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|Title:||Fascaplysin-inspired diindolyls as selective inhibitors of CDK4/cyclin D1.|
|Citation:||BIOORG MED CHEM, 2009, 17 (16), pp. 6073-6084|
|Abstract:||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.|
|Appears in Collections:||Published Articles, Dept. of Chemistry|
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