Author/Authors :
Carine Aubry، نويسنده , , A. James Wilson، نويسنده , , Daniel Emmerson، نويسنده , , Emma Murphy، نويسنده , , Yu Yam Chan، نويسنده , , Michael P. Dickens، نويسنده , , Marcos D. Garcia، نويسنده , , Paul R. Jenkins، نويسنده , , Sachin Mahale، نويسنده , , Bhabatosh Chaudhuri، نويسنده ,
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 IC50 for the best compounds 10m and 13a being 39 and 37 μm, respectively.
Keywords :
CDK4 inhibitors , Fascaplysin , Anti-cancer , Indoles
