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 ...