Assessment of metal-based dihydrofolate reductase inhibitors on a novel mesofluidic platform

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Polynuclear compounds are a relatively new and successful approach in metal-based cancer chemotherapy as typified by the trinuclear Pt compound BBR3464 which was evaluated in clinical trials. In this review, we discuss newer developments of polynuclear rut ...

The mechanism of action of sulfasalazine, an anti-inflammatory drug used against inflammatory bowel diseases and rheumatoid arthritis is, despite its medical importance, still not well understood. Recently, it was shown that sulfasalazine and its metabolit ...

Mycobacterium tuberculosis has a remarkable ability to persist within the human host as a clinically inapparent or chronically active infection. Fatty acids are thought to be an important carbon source used by the bacteria during long term infection. Catab ...

Hqpzc has been synthesized by a highly efficient procedure using the ionic liquid TBAB as an environmentally benign reaction medium. [Cu(qpzc)(OAc)]H2O (1) and [Zn(qpzc)(OAc)(H2O)] (2), complexes of the deprotonated ligand, qpzc [qpzc ...

A series of organometallic compds. of general formula [(arene)M(PTA)nXm]Y (arene = η6-C10H14, η-C5Me5); (M = Ru(II), Os(II), Rh(III) and Ir(III); X = Cl, mPTA; Y = OTf, PF6) have been screened for their cytotoxicity and ability to inhibit cathepsin B in vi ...

Metal complexes are increasingly being used to inhibit enzymes. The reasons for this increased interest arise from the special features that metal complexes offer, e.g. the facile construction of 3D architectures that tightly fill enzyme active sites incre ...

A review. Platinum complex-based chemotherapy is one of the major treatment options of many malignancies. Although severe side effects occur, and only a limited spectrum of tumors can be cured, Pt compds. are used in every second therapy scheme. Thus, many ...

Mass spectrometry (MS) has emerged as an important tool for studying anticancer metallodrugs in complex biological samples and for characterising their interactions with biomolecules and potential targets on a molecular level. The exact modes-of-action of ...

Enzymes that are involved in the synthesis and processing of oligosaccharides, such as glycosidases, are important catalysts for the specific assembly of oligosaccharide structures on proteins. Design and preparation of selective inhibitors of these enzyme ...

A series of cationic dinuclear p-cymene ruthenium complexes containing three thiolato bridges with different substituents at the sulfur atoms, (eta(6)-p-(MeC6H4Pr)-Pr-i)(2)Ru-2(mu(2)-SR1)(2)(mu(2)-SR2) (R-1 = CH2Ph, R-2 = Ph: 4; R-1 = CH2Ph, R-2 = p-( ...

Cisplatin is one of the most important and widely used anticancer drug in clinical use. However, its effectiveness is limited by its high toxicity and incidence of drug resistance. This has provided motivation for the search for transition metal-based drug ...

The first part of this thesis studies the problem of symmetry breaking in the context of simple mechanical systems with compact symmetry Lie group G. In this part we shall assume that the principal stratum of the G-action on the configuration space Q of a ...

The aim of this thesis was to explore the topoisomerase-DNA interactions using atomic force microscopy (AFM) in a liquid environment. Firstly, we present a programmable microcontroller-driven injection system for the exchange of an imaging medium while usi ...

Assessment of metal-based dihydrofolate reductase inhibitors on a novel mesofluidic platform

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