Fascaplysin-inspired diindolyls as selective inhibitors of CDK4/cyclin D1

Bioorg Med Chem. 2009 Aug 15;17(16):6073-84. doi: 10.1016/j.bmc.2009.06.070.

Carine Aubry ¹, A James Wilson, Daniel Emmerson, Emma Murphy, Yu Yam Chan, Michael P Dickens, Marcos D García, Paul R Jenkins, Sachin Mahale, Bhabatosh Chaudhuri

Affiliations

Affiliation

1 Department of Chemistry, University of Leicester, UK.

PMID: 19632122 DOI: 10.1016/j.bmc.2009.06.070

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.

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