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  • Design, synthesis and biological evaluation of new tryptamine and tetrahydro-beta-carboline-based selective inhibitors of CDK4.

Design, synthesis and biological evaluation of new tryptamine and tetrahydro-beta-carboline-based selective inhibitors of CDK4.

Bioorganic & medicinal chemistry (2008-07-25)
Paul R Jenkins, James Wilson, Daniel Emmerson, Marcos D Garcia, Matthew R Smith, Stephen J Gray, Robert G Britton, Sachin Mahale, Bhabatosh Chaudhuri
ABSTRACT

We present the design, synthesis and biological activity of a library of substituted (biphenylcarbonyl)-tryptamine and (biphenylcarbonyl)-tetrahydro-beta-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 IC(50) in the range 9-11 microM, three of them containing the para-biphenyl plus para-substituents supporting the existence of a pi-stacking pocket within the active site of CDK4.

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Millipore
Glutathione−Agarose, set of 3 pre-packed columns (2.5 ml each), (1:1 suspension in a 0.5 M NaCl + 20% ethanol solution)