Search results for "Complex."

Selected cytotoxic gold compounds cause significant inhibition of 20S proteasome catalytic activities

2014

Abstract Six structurally diverse cytotoxic gold compounds are reported to cause profound and differential inhibition of the three main catalytic activities of purified 20S proteasome whilst auranofin , an established gold(I) drug in clinical use, is nearly ineffective. In particular, the gold(I) complex [( pbiH ) Au ( PPh 3 )] PF 6 , turns out to be the most potent inhibitor of all three enzyme activities with sub-micromolar IC 50 values. The present results further support the view that proteasome inhibition may play a major – yet not exclusive – role in the cytotoxic actions of gold based anticancer agents.

Frontiers of metal-coordinating drug design

2020

INTRODUCTION: The occurrence of metal ions in biomolecules is required to exert vital cellular functions. Metal-containing biomolecules can be modulated by small-molecule inhibitors targeting their metal-moiety. As well, the discovery of cisplatin ushered the rational discovery of metal-containing-drugs. The use of both drug types exploiting metal–ligand interactions is well established to treat distinct pathologies. Therefore, characterizing and leveraging metal-coordinating drugs is a pivotal, yet challenging, part of medicinal chemistry. AREA COVERED: Atomic-level simulations are increasingly employed to overcome the challenges met by traditional drug-discovery approaches and to compleme…

Pectin as Drug-Release Vehicle

2020

Pectin as a natural biopolymer is extensively used for pharmaceutical and biomedical applications, essentially due to its gelling properties that could be influenced by pectin sources and extraction methods. This chapter focuses on an overview of pectin drug delivery systems classified by their administration routes. Oral drug delivery systems have been mainly developed, as pectin could be used in tablets as binder or matrix excipients and in microparticles/beads obtained by ionotropic gelation. The main objective is to target the colon, as pectin is resistant in acidic pH and sensitive to pectinolytic enzymes in the colon. To obtain suitable properties, pectin could be used in its native s…

Herbal hepatotoxicity: a hidden epidemic

2011

Complementary and alternative therapies, including herbal products, have become increasingly popular in the general population and among patients and physicians. Regulations and pharmacovigilance regarding herbal drugs are still incomplete and need to be improved. In fact, herbals are commonly marketed on the Internet, and in many countries they are sold as food supplements, which are beyond the control of drug regulatory agencies. In Europe and the U.S., reports of hepatotoxicity from these products, including those advertised for liver diseases, are accumulating. Many herbal drugs are also commonly used in children, and in women during pregnancy and lactation, because they are believed to…

Hexafluoro complex of rutherfordium in mixed HF/HNO3 solutions

2008

Formation of anionic fluoride-complexes of element 104, rutherfordium, produced in the 248 Cm( 18 O, 5n) 261 Rf reaction was studied by anion-exchange on an atom-at-a-time scale. It was found that the hexafluoro complex of Rf, [RfF 6 ] 2- , was formed in the studied fluoride ion concentrations of 0.0005-0.013 M. Formation of [RfF 6 ] 2- was significantly different from that of the homologues Zr and Hf, [ZrF 6 ] 2- and [HfF 6 ] 2- ; the evaluated formation constant of [RfF 6 ] 2- is at least one-order of magnitude smaller than those of [ZrF 6 ] 2- and [HfF 6 ] 2- .

Chemical studies on rutherfordium (Rf) at JAERI

2005

SummaryChemical studies on element 104, rutherfordium (Rf), at JAERI (Japan Atomic Energy Research Institute) are reviewed. The transactinide nuclide261Rf has been produced in the reaction248Cm(18O, 5n) at the JAERI tandem accelerator with the production cross section of about 13 nb. On-line anion-exchange experiments on Rf together with the lighter homologues, group-4 elements Zr and Hf, in acidic solutions have been conducted with a rapid ion-exchange separation apparatus. From the systematic study of the anion-exchange behavior of Rf, it has been found that the properties of Rf in HCl and HNO3solutions are quite similar to those of Zr and Hf, definitely confirming that Rf is a member of …

Duroquinone-Cyclopentadienyl-Cobalt

1963

Impulsively-controlled systems and reverse dwell time: A linear programming approach

2015

We present a receding horizon algorithm that converges to the exact solution in polynomial time for a class of optimal impulse control problems with uniformly distributed impulse instants and governed by so-called reverse dwell time conditions. The cost has two separate terms, one depending on time and the second monotonically decreasing on the state norm. The obtained results have both theoretical and practical relevance. From a theoretical perspective we prove certain geometrical properties of the discrete set of feasible solutions. From a practical standpoint, such properties reduce the computational burden and speed up the search for the optimum thus making the algorithm suitable for th…

Slow Relaxation of the Magnetization in Anilato-Based Dy(III) 2D Lattices.

2021

The search for two- and three-dimensional materials with slow relaxation of the magnetization (single-ion magnets, SIM and single-molecule magnets, SMM) has become a very active area in recent years. Here we show how it is possible to prepare two-dimensional SIMs by combining Dy(III) with two different anilato-type ligands (dianions of the 3,6-disubstituted-2,5-dihydroxy-1,4-benzoquinone: C6O4X22−, with X = H and Cl) in dimethyl sulfoxide (dmso). The two compounds prepared, formulated as: [Dy2(C6O4H2)3(dmso)2(H2O)2]·2dmso·18H2O (1) and [Dy2(C6O4Cl2)3(dmso)4]·2dmso·2H2O (2) show distorted hexagonal honeycomb layers with the solvent molecules (dmso and H2O) located in the interlayer space and…

Inferring slowly-changing dynamic gene-regulatory networks

2015

Dynamic gene-regulatory networks are complex since the interaction patterns between their components mean that it is impossible to study parts of the network in separation. This holistic character of gene-regulatory networks poses a real challenge to any type of modelling. Graphical models are a class of models that connect the network with a conditional independence relationships between random variables. By interpreting these random variables as gene activities and the conditional independence relationships as functional non-relatedness, graphical models have been used to describe gene-regulatory networks. Whereas the literature has been focused on static networks, most time-course experi…