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

Spencer, John, Casini, Angela ORCID: https://orcid.org/0000-0003-1599-9542, Zava, Olivier, Rathnam, Rajendra P., Velhanda, Santosh K., Pfeffer, Michel, Callear, Samantha K., Hursthouse, Michael B. and Dyson, Paul J. 2009. Excellent correlation between cathepsin B inhibition and cytotoxicity for a series of palladacycles. Dalton Transactions (48) , pp. 10731-10735. 10.1039/B912096C

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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.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Chemistry
Subjects:	Q Science > QD Chemistry
Publisher:	Royal Society of Chemistry
Date of Acceptance:	31 July 2009
Last Modified:	31 Oct 2022 08:58
URI:	https://orca.cardiff.ac.uk/id/eprint/79356

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