Synthesis of a 1,4-benzodiazepine containing palladacycle with in vitro anticancer and cathepsin B activity
| Autor: | Rajendra P. Rathnam, Arun K. Kotha, Michael B. Hursthouse, Simon C. W. Richardson, Louise Male, Ali Hazrati, Mahesh Motukuri, John A. Hartley, John Spencer |
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| Rok vydání: | 2009 |
| Předmět: |
Models
Molecular Magnetic Resonance Spectroscopy Cell Survival Stereochemistry chemistry.chemical_element Antineoplastic Agents Crystallography X-Ray Cathepsin B Inorganic Chemistry Benzodiazepines Inhibitory Concentration 50 chemistry.chemical_compound Cell Line Tumor Leukemia Myelogenous Chronic BCR-ABL Positive Chlorocebus aethiops Animals Humans Vero Cells Organometallic chemistry Cell Proliferation Molecular Structure Diphenylphosphine Chemistry Cell growth Nuclear magnetic resonance spectroscopy In vitro Liver Cell culture Drug Screening Assays Antitumor Palladium |
| Zdroj: | Dalton Transactions. :4299 |
| ISSN: | 1477-9234 1477-9226 |
| DOI: | 10.1039/b819061e |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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