- Fascaplysin-inspired diindolyls as selective inhibitors of CDK4/cyclin D1.
Fascaplysin-inspired diindolyls as selective inhibitors of CDK4/cyclin D1.
Bioorganic & medicinal chemistry (2009-07-28)
Carine Aubry, A James Wilson, Daniel Emmerson, Emma Murphy, Yu Yam Chan, Michael P Dickens, Marcos D García, Paul R Jenkins, Sachin Mahale, Bhabatosh Chaudhuri
PMID19632122
摘要
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.
