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Issue 22, 2009
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Synthesis of a 1,4-benzodiazepine containing palladacycle with in vitro anticancer and cathepsin B activity

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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. [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

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Publication details

The article was received on 28 Oct 2008, accepted on 24 Dec 2008 and first published on 29 Jan 2009


Article type: Paper
DOI: 10.1039/B819061E
Dalton Trans., 2009, 4299-4303

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    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

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