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Issue 5, 2006
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Design, synthesis and biological activity of new CDK4-specific inhibitors, based on fascaplysin

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Abstract

We present the design, synthesis, and biological activity of three classes of tryptamine derivatives, which are non-planar analogues of the toxic anti-cancer agent fascaplysin. We show these compounds to be selective inhibitors of CDK4 over CDK2, the most active compound 9q has an IC50 for the inhibition of CDK4 of 6 µM.

Graphical abstract: Design, synthesis and biological activity of new CDK4-specific inhibitors, based on fascaplysin

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Article information


Submitted
19 Dec 2005
Accepted
12 Jan 2006
First published
01 Feb 2006

Org. Biomol. Chem., 2006,4, 787-801
Article type
Paper

Design, synthesis and biological activity of new CDK4-specific inhibitors, based on fascaplysin

C. Aubry, A. J. Wilson, P. R. Jenkins, S. Mahale, B. Chaudhuri, J. Maréchal and M. J. Sutcliffe, Org. Biomol. Chem., 2006, 4, 787
DOI: 10.1039/B518019H

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