Issue 24, 2006
From the journal:

Organic & Biomolecular Chemistry

Synthesis, crystal structure and biological activity of β-carboline based selective CDK4-cyclin D1 inhibitors†

Marcos D. García,a   A. James Wilson,a   Daniel P. G. Emmerson,a   Paul R. Jenkins,*a   Sachin Mahaleb  and  Bhabatosh Chaudhurib  

* 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

Abstract

The design, synthesis and biological activity of a series of non-planar dihydro-β-carboline and β-carboline-based derivatives of the toxic anticancer agent fascaplysin is presented. We show these compounds to be selective inhibitors of CDK4 over CDK2 with an IC50 (CDK4-cyclin D1) = 11 µmol for the best compound in the series 4d. The crystallographic analysis of some of the compounds synthesised (3b/d and 4a–d) was carried out, in an effort to estimate the structural similarities between the designed inhibitors and the model compound fascaplysin.

Graphical abstract: Synthesis, crystal structure and biological activity of β-carboline based selective CDK4-cyclin D1 inhibitors

About
Cited by
Related
Download options Please wait...

Supplementary files

Article information

DOI
https://doi.org/10.1039/B613861F
Article type
Paper
Submitted
22 Sep 2006
Accepted
26 Oct 2006
First published
09 Nov 2006

Org. Biomol. Chem., 2006,4, 4478-4484

Permissions

Request permissions

Synthesis, crystal structure and biological activity of β-carboline based selective CDK4-cyclin D1 inhibitors

M. D. García, A. J. Wilson, D. P. G. Emmerson, P. R. Jenkins, S. Mahale and B. Chaudhuri, Org. Biomol. Chem., 2006, 4, 4478 DOI: 10.1039/B613861F

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements