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Oxaliplatin reacts with DMSO only in the presence of water

Paul Joseph Dyson, Laure Menin, Hristo Plamenov Varbanov

Herein we show that oxaliplatin reacts rapidly with DMSO in aqueous solutions, despite being stable in pure DMSO and pure water. Furthermore, the reactivity of the clinically applied Pt(II) drugs in water/DMSO and PBS/DMSO mixtures, and the nature of the s ...

2017

Optimization of drug combinations using Feedback System Control

Paul Joseph Dyson, Hubert van den Bergh, Patrycja Nowak-Sliwinska, Andrea Brett Gasser

We describe a protocol for the discovery of synergistic drug combinations for the treatment of disease. Synergistic drug combinations lead to the use of drugs at lower doses, which reduces side effects and can potentially lead to reduced drug resistance, w ...

Nature Publishing Group2016

Stabilization of the Amorphous Structure of Spray-Dried Drug Nanoparticles

Esther Amstad

The bioavailability of hydrophobic drugs strongly increases if they are formulated as amorphous materials because the solubility of the amorphous phase is much higher than that of the crystal. Moreover, the stability of these particles against crystallizat ...

Amer Chemical Soc2016

A streamlined search technology for identification of synergistic drug combinations

Paul Joseph Dyson, Hubert van den Bergh, Patrycja Nowak-Sliwinska, Andrea Brett Gasser

A major key to improvement of cancer therapy is the combination of drugs. Mixing drugs that already exist on the market may offer an attractive alternative. Here we report on a new model-based streamlined feedback system control (s-FSC) method, based on a ...

Nature Publishing Group2015

Crystallization of undercooled liquid fenofibrate

Esther Amstad

Formulation of hydrophobic drugs as amorphous materials is highly advantageous as this increases their solubility in water and therefore their bioavailability. However, many drugs have a high propensity to crystallize during production and storage, limitin ...

Royal Society of Chemistry2015

Chiral gamma-Lactams by Enantioselective Palladium(0)-Catalyzed Cyclopropane Functionalizations

Nicolai Cramer, Julia Pedroni

Cyclopropanes fused to pyrrolidines are important structural features found in a number of marketed drugs and development candidates. Typically, their synthesis involves the cyclopropanation of a dihydropyrrole precursor. Reported herein is a complementary ...

Wiley-VCH Verlag GmbH2015

Association of PCK1 with Body Mass Index and Other Metabolic Features in Patients With Psychotropic Treatments

Pierre Magistretti

Weight gain is a major health problem among psychiatric populations. It implicates several receptors and hormones involved in energy balance and metabolism. Phosphoenolpyruvate carboxykinase 1 is a rate-controlling enzyme involved in gluconeogenesis, glyce ...

Lippincott, Williams & Wilkins2015

Preclinical combination therapy of the investigational drug NAMI-A(+) with doxorubicin for mammary cancer

Paul Joseph Dyson, Tina Riedel

Aim of the study The tumor metastases targeting ruthenium complex NAMI-A synergistically improves the activity of gemcitabine in combination therapies. High-throughput screening was used to identify other potential drug combinations from a library of FDA a ...

Springer2015

Next-generation antimicrobials: from chemical biology to first-in-class drugs

Paul Murima

The global emergence of multi-drug resistant bacteria invokes an urgent and imperative necessity for the identification of novel antimicrobials. The general lack of success in progressing novel chemical entities from target-based drug screens have prompted ...

Pharmaceutical Soc Korea2015

Rapid optimization of drug combinations for the optimal angiostatic treatment of cancer

Paul Joseph Dyson, Hubert van den Bergh, Patrycja Nowak-Sliwinska, Andrea Brett Gasser

Drug combinations can improve angiostatic cancer treatment efficacy and enable the reduction of side effects and drug resistance. Combining drugs is non-trivial due to the high number of possibilities. We applied a feedback system control (FSC) technique w ...

2015

Discovery of benzothiazoles as antimycobacterial agents: Synthesis, structure-activity relationships and binding studies with Mycobacterium tuberculosis decaprenylphosphoryl-beta-D-ribose 2 '-oxidase

Stewart Cole, Florence Pojer, Joao Pedro De Almeida Neres, Anirban Ghosh

We report the discovery of benzothiazoles, a novel anti-mycobacterial series, identified from a whole cell based screening campaign. Benzothiazoles exert their bactericidal activity against Mycobacterium tuberculosis (Mtb) through potent inhibition of deca ...

Elsevier2015