2,254 research outputs found
Metal-based antitumour drugs in the post genomic era
No full textThe discovery of new metal-based antitumour drugs, whether cisplatin derivatives or those based on
other metals, has been largely based on cell viability assays (IC50 values) and compounds that bind to
DNA. This approach has been applied for more than 30 years during which time very few new drugs
have entered clinical use. In this article we discuss what the future holds for metal-based drugs, in
particular anti-metastasis drugs, in these enlightened times of the post genomic era
Styrene oxidation by hydrogen peroxide in ionic liquids: the role of the solvent on the competition between two Pd-catalyzed processes, oxidation and dimerization
No full textA series of hydrophilic N,N-dimethylpyrrolidinium-and N,N-dimethylpiperidinium-based ionic liquids (ILs) have been prepared and applied as reaction media in the Wacker oxidation of styrene by hydrogen peroxide using PdCl(2) as the catalyst. The efficiency of these ILs was compared with hydrophilic and hydrophobic imidazolium systems (including those with nitrile functionalities). The nature of the ionic liquid strongly influences the product distribution. In particular, in hydrophobic ILs, relevant amounts of 1,3-diphenyl-1-butene arising from styrene dimerization were detected, in addition to the expected phenylmethylketone. The formation of 1,3-diphenyl-1-butene may be attributed to the formation of Pd(0) species from "ClPdOH" (probably formed during the Wacker process) in a side-reaction. Consequently, the ability of the IL to favor or disfavor the reoxidation of "ClPdOH" to "ClPdOOH" by hydrogen peroxide, giving an homogeneous phase or a biphasic system, appears to be the main factor affecting selectivity
Preclinical combination therapy of the investigational drug NAMI-A with doxorubicin for mammary cancer
No full textAIM OF THE STUDY: The tumor metastases targeting ruthenium complex NAMI-A synergistically improves the activity of gemcitabine in combination therapies. High-throughput screening was used to identify other potential drug combinations from a library of FDA approved drugs. Doxorubicin was identified as a hit compound and was therefore evaluated in combination with NAMI-A in vitro and in a preclinical in vivo model.
RESULTS: High-throughput screening identified eight structurally diverse compounds that synergize with NAMI-A including doxorubicin. The combination index on MCF-7 cells showed synergism as the concentration of NAMI-A increases independent of the doxorubicin concentration. In MCa mammary carcinoma of CBA mice, NAMI-A (35 mg/kg/day i.p. on days 7-12) followed by doxorubicin (10 mg/kg i.p. on day 16), significantly increased the effects of the individual drugs on metastases with 70 % animals resulting free of macroscopically detectable tumor nodules in the lungs at sacrifice. NAMI-A, unlike doxorubicin, cured 60 % of the treated mice but the combination therapy was toxic to the animals.
CONCLUSIONS: The combined therapy of NAMI-A with doxorubicin synergizes on lung metastasis in a preclinical mouse model. The combination therapy at the maximum tolerated doses of the two drugs is toxic. Hence, this combination is not suitable for clinical studies using maximum tolerated doses
The role of cisplatin and NAMI-A plasma-protein interactions in relation to combination therapy
No full textModulation of the metastatic progression of breast cancer with an organometallic ruthenium compound
No full textThe synthesis, characterization and molecular structures of two mixed metal octahedral carbido clusters, Ru5RhC(CO)14(η5-C5Me5) and Ru5RhC(CO)9(η5-C5Me5)(η5-C5H5)2
No full textIonic coupling between the dianionic ruthenium cluster [Ru5C(CO14]2- and the dicationic rhodium species [Rh(C5 Me5)(MeCN)3]2+ in refluxing CH2Cl2 yields the hexanuclear mixed metal carbido cluster Ru5RhC(CO)14(eta5-C5Me5) (1). Activation of 1 towards reaction with C5H6 or C6H8 by trimethylamine-N-oxide (Me3NO) results in the formation of Ru5RhC (CO)9(eta5-C5Me5)(eta5-C5H5)2 (2) and Ru5RhC(CO)11(eta5-C5Me5)(mu3-eta2:eta2:eta2-C6H6) (3) respectively. Complexes 1 and 2 have been structurally characterized by X-ray diffraction
Remarkable anion and cation effects on Stille reactions in functionalised ionic liquids
No full textTask-specific ionic liquids bearing nitrile functional groups attached to the cation and nitrogen-donor-containing anions strongly affect the efficiency of the Stille cross-coupling, influencing, the nature of the catalyst and its stability. The relative strengths of the coordinating power of the cations and anions are varied and compared, and under certain conditions nanoparticles are observed
Organometallic ruthenium-based antitumor compounds with novel modes of action
No full text10.1016/j.jorganchem.2010.11.009Journal of Organometallic Chemistry6965989-998JORC
THE SYNTHESIS, STRUCTURAL CHARACTERIZATION AND VARIABLE-TEMPERATURE H-1-NMR STUDY OF THE BIS-TOLUENE HEXARUTHENIUM CARBIDOCARBONYL CLUSTER [RU6C(CO)(11)(ETA(6)-C(6)H(5)ME)(MU(3)-ETA(2)ETA(2)ETA(2)-C(6)H(5)ME)]
No full textThe synthesis, chemical characterisation and single crystal X-ray structural study of the bis-toluene hexaruthenium carbidocarbonyl cluster [Ru6C(CO)(1)1(eta(6)-C(6)H(5)Me)(mu(3)-eta(2):eta(2):eta(2)-C(6)H(5)Me)] is reported. A variable temperature H-1 n.m.r. study reveals that in solution the complex exists in two isomeric forms, one of them, that observed in the solid state and the solid state and the other the trans-[Ru6C(CO)(1)1(eta(6)-C(6)H(5)Me)(2)] isomer. Interchange of the toluene ligand between the mu(3)-eta(2):eta(2):eta(2) and eta(6) co-ordination mode if confirmed by deuterum labelling experiments involving C6D5CD3
SYNTHESIS, MOLECULAR AND CRYSTAL-STRUCTURES OF ARENE DERIVATIVES OF [RU6C(CO)17]
No full textThe complexes [Ru6C(CO)14(eta6-C6H4Me2-1,3)] 1, [Ru6C(CO)14(eta6CH3Et3-1,3,5)] 2 and [Ru6C-(CO)14(mu3-eta2:eta2:eta2-C16H16)] 3 have been prepared from the reaction of [Ru3(CO)12] and the appropriate arene. The molecular and crystal structures of the three derivatives have been established by single-crystal X-ray diffraction studies. Complexes 1 and 2 carry the arene fragment bound in a terminal fashion. Crystalline 1 contains two independent molecules showing different rotameric conformations of the xylene ligands. The [2.2]paracyclophane complex 3 provides the first example of a mono(arene) derivative of [Ru6C(CO)17] to contain the mu3-eta2:eta2:eta2-bonding mode. The molecular organization in the crystal structures of 1, 2 and 3 was also determined
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