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The title compound, [Ti(C11H21Si2)2(NH2)], crystallizes as a bent metallocene, with the NH2 group oriented to maximize the pi interaction between the N atom and the Ti(III) center. The increased pi bonding is reflected in a short Ti-N bond length of 1.933 (3) A.
Beyond its aromatic character and important hydrophobicity, cymantrenylalanine, a metallocenic amino-acid, can be easily photosubstituted with phosphine and phosphite ligands to readily yield new analogs with different hydrophobicity and steric hindrance. The incorporation of phosphine and phosphite ligands is described. As an illustration of the offered possibilities, the synthesis and the biological activity of two new GnRH analogs modified in position 6 are reported.
Uranium nitrides offer potential as future nuclear fuels and as probes of metal ligand multiple bonding involving the f-block actinide metals. However, few molecular examples are available for study owing to the difficulties in synthesis. Recent advances in organoactinide chemistry have provided a route to uranium nitride complexes that expands the options for developing UN chemistry. Several 24-membered uranium nitrogen rings, (UNUN3)4, have been synthesized by reduction of sodium azide with organometallic metallocene derivatives, [(C5Me4R)2U][(mu-Ph)2BPh2] (R = Me, H; Me = methyl, Ph = phenyl). The nanometer-sized rings contain unusual UNU nitride linkages that have short U-N distances within the double-bond range.
The quantitative analysis of binary polyethylene (PE) blends by Fourier transform infrared (FT-IR) spectroscopy has been achieved based on the ratio of two absorbance peaks in an FT-IR spectrum. The frequencies for the absorbance ratio are selected based on structural entities of the PE components in the blend. A linear relationship between the absorbance ratio and the blend composition was found to exist if one of the absorbance peaks is distinct to one of the components and the other peak is common to both components. It was also found that any peak resulting from short-chain branching in copolymers (such as linear low-density polyethylene (LLDPE) or metallocene-catalyzed LLDPE (mLLDPE)), is suitable for use as the peak that is designated as being distinct to that component. In order to optimize the linearity of the equation, however, the selection of the second common peak is the most important and depends on the blend system studied. Indeed, under certain circumstances peaks that are not spectrally distinct can be used successfully to apply the method. The method exhibits potential for the routine analysis of PE blends that have been calibrated prior to its application.
Major advances in our understanding of malaria parasite biology have been made. Coupled with the completion of the malaria genome, this has presented exciting opportunities for target-based antimalarial drug discovery. However, the unraveling of more validated biological targets will not necessarily translate into the identification of new chemical entities that are effective against drug resistant parasites in the long term. As history has already shown, development of antiplasmodial agents aimed at a single parasite target or specialized process has failed to stem the tide of drug resistance. This review highlights recent starting points and/or approaches to antimalarial drug discovery with particular emphasis on innovative efforts, which are not necessarily based on the identification of new drug targets and attendant inhibitor design. Approaches covered include utilization of validated chemical scaffolds, bioprecursor and carrier prodrugs, double drug development and/or multi-therapeutic strategies, use of metallocenic scaffolds, the medicinal chemistry of antimalarial natural products and in silico drug design.
A stereogenic center at the position beta to the metallocene backbone is present in ferrocenyl ligands 2, which are interesting for asymmetric catalysis. These planar-chiral compounds are accessible for the first time by a highly diastereoselective and enantioselective synthesis (de=93-97 %; ee>/=96 %) from the ferrocenyl ketones 1. A variety of donor groups (E(1)=Ph(2)P small middle dotBH(3), SMe, SiPr; E(2)=SMe, STol, SePh, Ph(2)P small middle dotBH(3), iPr(2)P small middle dotBH(3)) can be introduced as electrophiles. Tol=tolyl=CH(3)C(6)H(4).
The antitumor activity of molybdocene dichloride is tested against Ehrlich ascites tumor in CF1 mice. The application of 75 of 100 mg/kg 24 h after transplantation achieves 100% tumor inhibition until day 30. Following the d0 and d1 metallocene dichlorides of titanium and vanadium, molybdocene dichloride is the first analogous d2 system revealing similar antineoplastic properties.
Evidence is presented in support of an electron transfer mechanism for various metal complexes possessing anti-neoplastic properties. Cyclic voltammetry was performed on several metallocenes, bis(acetato)bis(imidazole)Cu(II), and coordination compounds (Cu or Fe) of the antitumor agents, bipyridine, phenanthroline, hydroxyurea, diethyldithiocarbamate, and alpha, alpha'-bis(8-hydroxyquinolin-7-yl)-4-methoxytoluene. The favorable reduction potentials ranged from +0.5 to -0.5 Electrochemical behavior is correlated in some cases with structure and physiological activity. Relevant literature data are discussed.
Cisplatin, Carboplatin and new compounds such as Paclitaxel and Docetaxel are effective drugs in the treatment of ovarian cancer. Multidrug resistance however remains an issue in ovarian cancer. The search for new effective drugs will remain of the highest priority in the field of cancer research. The in vitro and in vivo growth inhibiting potencies of two new metallocene dichlorides, Titanocendichloride and Vanadocendichloride, were compared to Cisplatin and Carboplatin using 20 permanent human ovarian cancer cell lines. Under in vivo and in vitro conditions Cisplatin was more effective than Carboplatin. Under in vitro conditions a Vanadocendichloride concentration of as low as 1.5 x 10(-7) mol/l resulted in a 50% decrease in the cell proliferation. Titanocendichloride inhibited cellular growth only at concentrations of 10(-4) mol/l. In contrast, Titanocendichloride was more effective in inhibiting growth of xenotransplanted ovarian cancer cell lines in nude mice. The clinically supposed equipotentiality of Carboplatin should be handled cautiously. The new organometallic substances clearly exhibit antiproliferative properties in ovarian cancer cells and are considered for clinical phase I trials.
Ferrocene-A (ferrocenyl-1-phenyl-1-dioxy-1,4-butin-2) has shown significant antitumour and antibacterial activity. To facilitate studies in this field a simple and rapid liquid chromatographic procedure was developed, allowing the determination of ferrocene-A in the blood serum. The procedure was based on a reversed-phase high-performance liquid chromatography (HPLC) method, with UV detection at 210 nm. The mobile phase ethanol-0.01 M KH2PO4 60:40 (v/v) provides the complete separation of ferrocene-A, internal standard and endogenous compounds of serum. The recovery of ferrocene-A from serum using a hexaneisoamyl alcohol mixture was 90%. The proposed method is convenient for pharmacological and pharmacokinetic applications.
A tandem electrospray mass spectrometric (MS(n)) technique for the analysis of N-acetylated hexose carbohydrates using ferrocene boronate (F(c)Bor) derivatization was developed. The biologically important N-acetyl hexosamines can be readily distinguished utilizing this technique. The analysis is made possible by utilizing the inherent electrochemical properties of the electrospray device to produce oxidized, pre-formed single-electron ferrocenyl ions in a non-aqueous solvent system. The electrospray device was modified using a custom built cell consisting of concentric stainless steel tubes, which produced an enhanced signal for the molecular ion of each analyte species. The MS(2) spectra derived from isomeric populations of ferrocenyl boronic esters of these carbohydrates when generated under the same conditions possessed features unique to each sugar allowing easy differentiation between a number of N-acetyl hexosamine isomers.
Aliphatic amines, incorporating one or three (branched) acylated beta-D-glucopyranosyl residues, were coupled with the acid chloride of ferrocenecarboxylic acid and with the diacid chloride of 1,1'-ferrocenedicarboxylic acid to afford four dendrimer-type, carbohydrate-coated ferrocene derivatives in good yields (54-92%). Deprotection of the peracylated beta-D-glucopyranosyl residues was achieved quantitatively by using Zemplén conditions, affording four water-soluble ferrocene derivatives. When only one of the two cyclopentadienyl rings of the ferrocene unit is substituted, strong complexes are formed with beta-cyclodextrin in H2O, as demonstrated by liquid secondary ion mass spectrometry (LSIMS), 1H NMR spectroscopy, electrochemical measurements, and circular dichroism spectroscopy. Molecular dynamics calculations showed that the unsubstituted cyclopentadienyl ring is inserted through the cavity of the toroidal host in these complexes. The electrochemical behavior of the protected and deprotected ferrocene-containing dendrimers was investigated in acetonitrile and water, respectively. The diffusion coefficient decreases with increasing molecular weight of the compound. The potential for oxidation of the ferrocene core, the rate constant of heterogeneous electron transfer, and the rate constant for the energy-transfer reaction with the luminescent excited state of the [Ru(bpy)3]2+ complex (bpy = 2,2'-bipyridine) are strongly affected by the number (one or two) of substituents and by the number (one or three) of carbohydrate branches present in the substituents. These effects are assigned to shielding of the ferrocene core by the dendritic branches. Electrochemical evidence for the existence of different conformers for one of the dendrimers in aqueous solution was obtained.
A new chip-based electrochemical immunoassay protocol, based on the use of a ferrocene redox label, is described. Two reaction formats, based on direct (noncompetitive) and competitive modes of operation, were employed for illustrating the use of redox tracers in chip-based electrochemical immunoassays. The direct assay consisted of mixing the ferrocene-tagged antibody and the antigen analyte, a rapid electrophoretic separation of labeled free antibody and the labeled antigen/antibody complex, and a downstream anodic detection of the ferrocene tracer at gold-plated carbon screen-printed electrode detector. The competitive assay integrates precolumn reactions of the labeled antigen and the target antigen with the antibody with electrophoretic separation of the free and bound labeled antigens, along with amperometric detection of the redox tag. An internal standard has been used to normalize the peak area for the construction of calibration plots. Fundamental operating variables are examined and optimized. The use of a redox tracer offers the advantages of simplified protocol, wider linear range, higher stability, and higher separation efficiency compared to an analogous use of enzyme tags. The direct mouse-immunoglobulin G (IgG) assay and the competitive 3,3',5-triiodo-L-thyronine (T(3)) one were accomplished within less than 150 and 130 s (with field strengths of 256 and 192 V/cm), and offer minimum detectable concentrations of 2.5 x 10(-12) and 1 x1 0(-6) g/mL, respectively. Such use of redox labels for chip-based amperometric immunoassay protocols offers considerable promise for decentralized clinical or environmental testing.
The preparation of a gold electrode modified by ferrocenecarboxylic acid (FcA) covalently bound to L-cysteine self-assembled monolayer (FcA-SAM) is described. The modified electrode shows an excellent electrocatalytic activity for the oxidation of hydroquinone (QH2) and accelerates the electron transfer rate. The anodic overpotential is reduced by ca. 290 mV compared to those obtained at bare gold electrodes. The charge transfer coefficient and the apparent surface electron transfer rate constant for the redox couple of Q/QH2 at the modified electrode are found to be 0.425 and 0.96 s(-1), respectively. The catalytic current response of DPV increases linearly with the QH2 concentration from 5.7 x 10(-7) to 3.2 x 10(-4) M. The estimation of QH2 in a simulative sample is satisfactory. The method is simple, quick, and sensitive.
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