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

Spencer, John, Rathnam, Rajendra P, Motukuri, Mahesh, Kotha, Arun K, Richardson, Simon C W, Hazrati, Ali, Hartley, John A, Male, Louise and Hursthouse, Michael B (2009) Synthesis of a 1,4-benzodiazepine containing palladacycle with in vitro anticancer and cathepsin B activity. Dalton Transactions, 38 (22). pp. 4299-4303. ISSN 1477-9226

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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. [Pd(2)L(2)(mu-dppe)Cl(2)] 3, which was characterised in solution by (1)H and (31)P 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 IC(50) value of 4.3 microM (1 h exposure) and displayed cathepsin B inhibitory action with an IC(50) value of 3 microM.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Subjects: Q Science
Depositing User: Deeptima Massey
Date Deposited: 22 Oct 2012 13:21
Last Modified: 02 Jul 2013 13:19
URI: http://sro.sussex.ac.uk/id/eprint/40943
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