Synthesis and Characterization of New Ethylenediamine Platinum(IV) Complexes Containing Lipophilic Carboxylate Ligands

A series of new ethylenediamine (en) platinum(IV) complexes of the type Pt(IV)enX2A2, with X2  = cyclobutane-1,1-dicarboxylato (CBDCA), dichloro or bis(decanoato) and A = acetato, dodecanoato, tetradecanoato, hexadecanoato, octadecanoato, adamantanecarboxylato (Ad) or 3α, 12α-diformoxy-5β-cholato (DFCA) were synthesized and characterized by elemental analysis, infrared and NMR (1H  and  13C) spectroscopic techniques. Previous platinum(IV) compounds were usually restricted to trans-dihydroxo or trans-dichloro platinum(IV) complexes. Recently trans-dicarboxylato platinum(IV) complexes with mainly acetate, trifluoracetate or short-chain carboxylate groups (<11 carbons) in the axial position have been described in the literature[1,2,3]. In this paper we report on the synthesis and characterization of a new class of ethylenediamine platinum(IV) compounds that have high lipophilic long-chain carboxylate ligands either in the axial or equatorial position. The platinum(IV) compounds with the lipophilic trans-carboxylate ligands in the axial position were prepared by acylation of the trans-dihydroxo platinum(IV) species using an acyl halide in the presence of pyridine. In contrast to previous publications[1] the yields were excellent (up to 94%!)

Offensive Motivation Strategies: The Managerial And Legal Implications

This case study focuses on corporate culture, ethics, employment law, and motivation theory and is appropriate for use in a variety of management classes, such as organizational behavior, human resource management, or ethics.&nbsp; It profiles a lawsuit brought against a company by one of its female employees who was subjected to a variety of &ldquo;camaraderie building&rdquo; exercises, including being spanked with a competitor&rsquo;s metal poled yard sign.&nbsp; The case is based on a true story.&nbsp; Only the names and locations have been changed. &nbsp;This case includes actual&nbsp;descriptions of company practices and communications which are offensive and may be disturbing.&nbsp; However,&nbsp;they have been included&nbsp;so that the reader can appreciate the&nbsp;severity&nbsp;of the &ldquo;motivational practices&rdquo; that were being employed. &nbsp

Synthesis of (N,N'-Bis(2-Hydroxyethyl)Ethane-1,2-Diamine)Malonatoplatinum(II) and X-Ray Crystal Structure of the Cis-R,S-Isomer

Hydroxyethyl substituted amineplatinum(II) and (IV) complexes are an interesting class of platinum based antitumour compounds due to their uncoordinated hydroxy groups. These hydroxy groups could play an important role in the mode of action of such complexes with respect to their ability to act as donor or acceptor for hydrogen bonds. Moreover, their chemistry in solution is of interest because it was found that there is the possibility of an intramolecular attack to form ethanolatoamine chelated species which are responsible for very stable monoadducts with 5'-GMP. Furthermore, there is the possibility of derivatisation at the OH site to form a new series of platinum compounds which may be used for a carrier mediated transport to tumour tissues. In this context a series of (N,N'-bis(2-hydroxyethyl)ethane-l,2-diamine)-platinum(II) complexes has been synthesised. During purification of one of the platinum based compounds, it was possible to isolate (SP-4-3)-R,S-(N,N'-bis(2-hydroxyethyl)ethane-l,2-diamine)malonatoplatinum(ll) and to resolve the structure by single crystal structure analysis. Intra- and intermolecular hydrogen bonds have been found which may explain the spontaneous crystallisation of the cis-R,S isomer and the stabilisation of the boat conformation of the malonatoplatinum(II) six-membered ring

The binding properties of two antitumor ruthenium(III) complexes to apotransferrin.

The interaction of two ruthenium(III) complexes exhibiting high anticancer activity, namely trans-indazolium(bisindazole)tetrachlororuthenate(III) (ru-ind) and trans-imidazolium(bisimidazole)tetrachlororuthenate(III) (ru-im), with human serum apotransferrin has been investigated through spectroscopic and chromatographic techniques with the ultimate goal of preparing adducts with good selectivity for cancer cells. Whereas the binding of ru-im to human serum apotransferrin takes several hours, ru-ind, the less toxic complex, gives rise to a well defined 2:1 complex within a few minutes. We have ascertained that ru-ind binding occurs around the iron binding sites; binding does not occur in the absence of bicarbonate, and this anion dictates the kinetic and mechanistic characteristics of protein binding of ru-ind. The two ruthenium(III) complexes do not behave as iron(III) complexes, e.g. Fe(EDTA) or Fe(nitrilotriacetate), which lose their respective ligands when binding apotransferrin, but the N-heterocycles remain attached to the metal in the protein-bound species. Reversion of binding is obtained by acidification in the presence of chelators such as citrate or ATP. In comparison with cisplatin and its deactivation by serum proteins, our results indicate that other metal complexes such as ru-ind could use transferrin as a drug delivery system. Furthermore, the rapid protein binding of ru-ind seems to be related to a lower toxicity while still exhibiting high antitumor activity

Wie viel Arbeit macht die Aufzucht von Ökologischen Junghennen? Arbeitwirtschaftlicher Vergleich der konventionellen und ökologischen Aufzucht von Legehennen

Organic pullets are reared with daylight and are not beak-trimmed. Therefore, certain provisions are needed in order to prevent feather-pecking and cannibalism. Respec-tive guidelines are set by the German Organic Associations. It was the goal of this study to investigate whether the higher rearing standards are associated with an increased labour demand compared to conventional rearing systems. Using a ques-tionnaire, data from 32 hen-houses (10 conventional and 6 organic barn systems, 10 conventional and 6 organic aviary systems) about duration and number of working procedures were collected and exemplary models calculated. Total labour demand was between 2.36 and 7.37 worker`s hours/100 pullets. It did not differ between or-ganic and conventional rearing when comparing similar flock sizes, but were partly differently allocated to the different working procedures. On average, organic farms had smaller flocks, and there was a large influence of flock size on labour demand with small houses requiring most labour per hen. Also aviaries were more labour demanding than barn systems, but were usually associated with higher flock sizes. Our results indicate that improved pullet rearing that allows the birds to perform their natural behaviour more completely, does not necessarily cause higher labour re-quirements

Clec9a-mediated ablation of conventional dendritic cells suggests a lymphoid path to generating dendritic cells In Vivo

Conventional dendritic cells (cDCs) are versatile activators of immune responses that develop as part of the myeloid lineage downstream of hematopoietic stem cells. We have recently shown that in mice precursors of cDCs, but not of other leukocytes, are marked by expression of DNGR-1/CLEC9A. To genetically deplete DNGR-1-expressing cDC precursors and their progeny, we crossed Clec9a-Cre mice to Rosa-lox-STOP-lox-diphtheria toxin (DTA) mice. These mice develop signs of age-dependent myeloproliferative disease, as has been observed in other DC-deficient mouse models. However, despite efficient depletion of cDC progenitors in these mice, cells with phenotypic characteristics of cDCs populate the spleen. These cells are functionally and transcriptionally similar to cDCs in wild type control mice but show somatic rearrangements of Ig-heavy chain genes, characteristic of lymphoid origin cells. Our studies reveal a previously unappreciated developmental heterogeneity of cDCs and suggest that the lymphoid lineage can generate cells with features of cDCs when myeloid cDC progenitors are impaired