Insertion of (Bioactive) Equatorial Ligands into Platinum(IV) Complexes

Platinum(IV) prodrugs are highly interesting alternatives to platinum(II) anticancer therapeutics due to their increased tumor selectivity and reduced side effects. In contrast to the established theory, we recently observed that the equatorial ligand(s) of e.g. oxaliplatin(IV) complexes can be hydrolyzed with formation of [(DACH)Pt(OH_eq)₂(OAc_ax)₂]. In the work presented here, we investigated the reactivity and synthetic usability of this complex to be exploited as a precursor for the development of novel platinum(IV) complexes, not able to be synthesized by conventional protocols. Indeed, we could substitute the equatorial hydroxido ligand(s) e.g. by one or two monodentate biotin ligands (which would be oxidized under standard methods). The formed complexes turned out to be very stable with slow ligand release after reduction, ideal for long-circulating tumor-targeting strategies. Therefore, two platinum(IV) complexes with equatorial maleimides, capable of exploiting serum albumin as a natural nanocarrier, were synthesized as well. The complexes showed massively prolonged plasma half-life and distinctly improved anticancer activity in vivo compared to oxaliplatin. Taken together, the newly developed synthetic platform allows the simple and specific insertion of equatorial ligands into platinum(IV) complexes. This will enable the attachment of three different (bioactive) moieties generating targeted triple-action platinum(IV) prodrugs within one single platinum complex.     

Antiparasitic activities of bimetallic N-heterocyclic carbene gold(I) complexes with ferrocene ligands: Relevance of chlorido and phosphino ligands

Gold(I) complexes carrying imidazole-2-ylidene ligands and ferrocene substituents were prepared. Their activities against protozoal Leishmania major and Toxoplasma gondii parasites were analyzed. Certain gold(I) complexes with chlorido and 1,1′-bis(triphenylphosphino)ferrocene ligands revealed promising antiparasitic effects. The new chlorido complexes 5b and 5c showed high activities against T. gondii tachyzoites and L. major promastigotes while the new ferrocene-bridged bis-gold(I) complexes 8a and 8b were particularly active against L. major amastigotes and considerably selective as to toxicity results from Vero cells and macrophages.     

Extremal Rational Functions on Symmetric Discrete Sets and Superlinear Convergence of the ADI Method

There is a very fruitful interaction between numerical linear algebra and logarithmic potential theory. For instance, we may describe weak asympotics for a polynomial extremal problem occurring in the convergence analysis of conjugate gradients (CG) or of Ritz values; here the link with a constrained minimal energy problem allows to quantify the effect of superlinear convergence.     

Smooth Fréchet globalizations of Harish-Chandra modules

We give an alternative proof of the Casselman-Wallach globalization theorem. The approach is based on lower bounds for matrix coefficients on a reductive group.     

Trialkylaluminum N-Heterocyclic Olefin (NHO) Adducts as Catalysts for the Polymerization of Michael-Type Monomers

The synthesis of new trialkylaluminum adducts with N-heterocyclic olefin (NHO) ligands is described. These well-defined complexes can catalyze the polymerization of various Michael-type monomers, such as 2-vinylpyridine, methylacrylate, and dimethylacrylamide.     

Informational inefficiency in financial markets

The existence of an informational inefficiency in the equity market is identified by analysing information publicly available on the internet. A large volume of blog data is used for this purpose. Informational inefficiency is established by converting company-specific blog sentiment data into a trading strategy and analysing its performance. An information-based model that approximately replicates the strategy is developed to estimate the degree of information disparity. The result shows that an efficient internet search engine can considerably enhance market efficiency, as measured in terms of the information flow rate.     

A remark on a theorem by Claire Amiot

Claire Amiot has classified the connected triangulated k-categories with finitely many isoclasses of indecomposables satisfying suitable hypotheses. We remark that her proof shows that these triangulated categories are determined by their underlying k-linear categories. We observe that, if the connectedness assumption is dropped, the triangulated categories are still determined by their underlying k-categories together with the action of the suspension functor on the set of isoclasses of indecomposables.