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Title: Fascaplysin-inspired diindolyls as selective inhibitors of CDK4/cyclin D1.
Authors: Aubry, C
Wilson, AJ
Emmerson, D
Murphy, E
Chan, YY
Dickens, MP
García, MD
Jenkins, PR
Mahale, S
Chaudhuri, B
First Published: 15-Aug-2009
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.
DOI Link: 10.1016/j.bmc.2009.06.070
eISSN: 1464-3391
Type: Journal Article
Appears in Collections:Published Articles, Dept. of Chemistry

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