Issue 22, 2009
From the journal:

Dalton Transactions

Synthesis of a 1,4-benzodiazepine containing palladacycle with in vitro anticancer and cathepsin B activity†

John Spencer,*a   Rajendra P. Rathnam,a   Mahesh Motukuri,a   Arun K. Kotha,a   Simon C. W. Richardson,a   Ali Hazrati,b   John A. Hartley,b   Louise Malec  and  Michael B. Hursthousec  

* Corresponding authors

a School of Science, University of Greenwich at Medway, Chatham Maritime, UK
E-mail: j.spencer@gre.ac.uk
Fax: +44 (0)208 331 9805

b Cancer Research UK Drug-DNA Interactions Research Group, UCL Cancer Institute, Paul O'Gorman Building, 72 Huntley Street, University College London, UK

c EPSRC National Crystallography Service, School of Chemistry, University of Southampton, Highfield, Southampton, UK

Abstract

The reaction of the five-membered C,N-palladacycle [(L)PdCl]2, where LH = 1-methyl-5-phenyl-1H-1,4-benzodiazepin-2(3H)-one, with 1,2-ethanebis(diphenylphosphine), dppe, leads to the formation of the bridged palladacycle. [Pd2L2(μ-dppe)Cl2] 3, which was characterised in solution by 1H and 31P NMR spectroscopy and in the solid state by X-ray crystallography. Complex 3 was tested in vitro against a number of cell lines. For example, it inhibited K562 leukaemia cells with an IC50 value of 4.3 μM (1 h exposure) and displayed cathepsin B inhibitory action with an IC50 value of 3 μM.

Graphical abstract: Synthesis of a 1,4-benzodiazepine containing palladacycle with in vitro anticancer and cathepsin B activity

About
Cited by
Related
Download options Please wait...

Supplementary files

Article information

DOI
https://doi.org/10.1039/B819061E
Article type
Paper
Submitted
28 Oct 2008
Accepted
24 Dec 2008
First published
29 Jan 2009

Dalton Trans., 2009, 4299-4303

Permissions

Request permissions

Synthesis of a 1,4-benzodiazepine containing palladacycle with in vitro anticancer and cathepsin B activity

J. Spencer, R. P. Rathnam, M. Motukuri, A. K. Kotha, S. C. W. Richardson, A. Hazrati, J. A. Hartley, L. Male and M. B. Hursthouse, Dalton Trans., 2009, 4299 DOI: 10.1039/B819061E

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