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Issue 48, 2009
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Excellent correlation between cathepsin B inhibition and cytotoxicity for a series of palladacycles

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Abstract

The reaction of the five- or six-membered C,N or C,S-palladacycles [(L)PdCl]2 with PTA (1,3,5-triaza-7-phosphaadamantane) led to the monomeric complexes [(L)Pd(PTA)Cl] 6a, 6b and 7 where LH= N,N-dimethyl-1-phenylmethanamine, benzyl(methyl)sulfane or 1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one respectively. Dimeric complexes have also been synthesised: [Pd2L2(μ-dppe)Cl2], where LH = 1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one (1a), (R)- or (S)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one (1b, 1c), [Pd2L2(μ-dppf)Cl2], where L= 1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one (4a) or (R)-3-isopropyl-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one (4b), respectively, and dppe = 1,2-bis(diphenylphosphino)ethane, dppf = 1,1′-bis(diphenylphosphino)ferrocene. The complexes were characterised in solution, by 1H and 31P NMR spectroscopy, and single crystals of complexes 6b and 7 were studied in the solid state by X-ray crystallography. The palladacycles were evaluated for in vitro activity as cytotoxic agents on A2780/S cells and also as cathepsin B inhibitors, an enzyme implicated in a number of cancer related events.

Graphical abstract: Excellent correlation between cathepsin B inhibition and cytotoxicity for a series of palladacycles

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Publication details

The article was received on 19 Jun 2009, accepted on 31 Jul 2009 and first published on 24 Aug 2009


Article type: Paper
DOI: 10.1039/B912096C
Citation: Dalton Trans., 2009,0, 10731-10735
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    Excellent correlation between cathepsin B inhibition and cytotoxicity for a series of palladacycles

    J. Spencer, A. Casini, O. Zava, R. P. Rathnam, S. K. Velhanda, M. Pfeffer, S. K. Callear, M. B. Hursthouse and P. J. Dyson, Dalton Trans., 2009, 0, 10731
    DOI: 10.1039/B912096C

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