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Title: Design, synthesis and biological evaluation of new tryptamine and tetrahydro-beta-carboline-based selective inhibitors of CDK4.
Authors: Jenkins, PR
Wilson, J
Emmerson, D
Garcia, MD
Smith, MR
Gray, SJ
Britton, RG
Mahale, S
Chaudhuri, B
First Published: 15-Aug-2008
Citation: BIOORG MED CHEM, 2008, 16 (16), pp. 7728-7739
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.
DOI Link: 10.1016/j.bmc.2008.07.002
eISSN: 1464-3391
Type: Journal Article
Appears in Collections:Published Articles, Dept. of Chemistry

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