1063171-05-0Relevant articles and documents
Design, synthesis and biological evaluation of new tryptamine and tetrahydro-β-carboline-based selective inhibitors of CDK4
Jenkins, Paul R.,Wilson, James,Emmerson, Daniel,Garcia, Marcos D.,Smith, Matthew R.,Gray, Stephen J.,Britton, Robert G.,Mahale, Sachin,Chaudhuri, Bhabatosh
, p. 7728 - 7739 (2008)
We present the design, synthesis and biological activity of a library of substituted (biphenylcarbonyl)-tryptamine and (biphenylcarbonyl)-tetrahydro-β-carboline compounds related to the natural product fascaplysin, as novel inhibitors of CDK4/cyclin D1. We show all these molecules, prepared using the Suzuki-Miyaura reaction, being selective inhibitors of CDK4 over CDK2. The most active compounds have a CDK4 IC50 in the range 9-11 μM, three of them containing the para-biphenyl plus para-substituents supporting the existence of a π-stacking pocket within the active site of CDK4.
