Issue 5, 2006
From the journal:

Organic & Biomolecular Chemistry

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

Carine Aubry,a   A. James Wilson,a   Paul R. Jenkins,*a   Sachin Mahale,b   Bhabatosh Chaudhuri,b   Jean-Didier Maréchal†c  and  Michael J. Sutcliffe‡c  

* Corresponding authors

a Department of Chemistry, University of Leicester, Leicester, UK
E-mail: kin@le.ac.uk
Fax: +44(0)116 252 3789
Tel: +44(0)116 252 2124

b School of Pharmacy, De Montfort University, Leicester, UK
E-mail: bchaudhuri@dmu.ac.uk
Fax: +44(0)116 257 7287
Tel: +44(0)116 250 7280

c Departments of Biochemistry and Chemistry, University of Leicester, Leicester, UK

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

DOI
https://doi.org/10.1039/B518019H
Article type
Paper
Submitted
19 Dec 2005
Accepted
12 Jan 2006
First published
01 Feb 2006

Org. Biomol. Chem., 2006,4, 787-801

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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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