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SOME BIOLOGICAL PROPERTIES OF TRITERPENOID ACIDS
S.N. Morozkina, O.I. Antimonova, E.M. Eremenko*, A.G. Shavva

Ursolic and betulinic acids acids induce the processes of apoptosis. We tested the risk of osteoporosis induction under influence of triterpenoids, since they can interact with glucocorticoid receptors. In experiments on oviriectomized rats we found that acids do not show any negative influence on percentage of mineral components in the femur and have cholesterol-lowering action under experimental conditions.

THE OSTEOPROTECTIVE ACTION OF 6-OXA-8a-ANALOGUES OF STEROID ESTROGENS
A.G. Shavva, V.N. Belov, A.Yu. Solovyev, S.N. Morozkina

We synthesized fourteen 6-oxa-8a-estrogens analogues and investigated osteoprotective and uterotropic actions. We demonstrated correlation: every modification in structure of 6-oxa-8-analogues leading to strong (>30%) reduction of uterotropic action induces slump of osteoprotective activity. This allows to make conclusion: main biotarget, responsible for appearance of osteoprotective action is a-estrogen receptor. We found steroid estrogen analogues with cholesterol-lowering properties without u

Scalability of heterogeneous MW-heated processes
Mark H.C.L. Dressen, Bastiaan H. P. van de Kruijs, Jan Meuldijk, Jef A. J. M. Vekemans, Lumbertus A. Hulshof

The combination of flow chemistry and microwave heating offers a unique opportunity to scale out heterogeneous microwave-assisted organic reactions. The feasibility of this setup is depending on the presence of a microwave effect, safety issues and energy efficiency.

A Modular Solution for Storage of Biological Samples
Joby Jenkins, Wayne Bowen, Ben Schenker, Chloe Milburn

The physical and chemical composition of biological samples is more diverse than the libraries of medicinal compounds used for drug discovery research. Types of samples include proteins, nucleic acids, blood and serum samples, cell suspensions, tissue biopsies, and antibodies. Thus any storage system must be flexible to accommodate the differing storage requirements of each sample type base upon its biochemical composition, stability and where appropriate, solvent.

Low Volume Liquid Handling of Organic Solvents for Compound Storage and Dissolution using mosquito
Gillian Lewis, Tristan Cope, Joby Jenkins, David Gledhill & Rob Lewis

mosquito® is a positive displacement liquid handling system capable of pipetting solutions with a high degree of accuracy (to within 5%) and precision (CVs of <10%) in the nanolitre range. Here, we demonstrate mosquito’s ability to dispense accurately low volumes of organic solvents of low surface tension and to re-dissolve compounds which have been previously dried in storage wells.

Palladium-Catalyzed Three-Component Synthesis of Phenothiazines
Troels Dahl, Christian Wenzel Tornøe, Benny Bang-Andersen, Poul Nielsen and Morten Jørgensen

The formation of aromatic carbon-heteroatom bonds has traditionally been achieved by nucleophilic aromatic substitution or via the copper-mediated Ullman reaction. The palladium-catalyzed formation of aromatic C-N bonds extensively developed by Hartwig and Buchwald has provided a powerful alternative. While the aryl amination reaction is applicable even to aryl chlorides and activated phenols, the analogous C-O and C-S bond forming reactions have attracted less attention.

Combinatorial synthesis of oxazolidin-2-ones using Fmoc-Ser(Trt)-OH, a library with high degree of diversity
Marek Korinek, Vaclav Stastny and Miroslav Havranek

A library of oxazolidin-2-ones was prepared by solid phase synthesis. Crutial reaction steps were optimized. Highly divers building blocks were selected for the synthesis. All compounds were purified using preparative LC/MS with mass directed fraction collection.

High Throughput Surface Tension Measurement
Neil L. Campbell, Jon Weaver

Understanding the surface tension properties of aqueous surfactants and polymer materials is important for the pharmaceutical, coatings, paints, inks, surfactant and household products industries. The traditional methods of measuring surface tension are tedious and time-consuming, so only a few compounds can be measured by a single user per day.

High Throughput Microwave Synthesis of Metal Organic Framework (MOF) Libraries
Neil L. Campbell, Jake Grace, Richard W. Dewson, Jean-Noel Rebilly, Darren Bradshaw, Ben Carter, Andrew I. Cooper and Mathew J. Rosseinsky

Metal-organic frameworks (MOFs) are an emerging class of new nano-porous materials of considerable academic and industrial interest due to their potential applications in gas storagechiral separations and catalysis. MOFs are prepared from the self-assembly of metal ions (nodes) and organic ligands (spacers), where the structural topology of the resulting crystalline frameworks is driven by the co-ordination preferences of these nodes and spacers. MOFs offer opportunities not available to more cl

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Showing Results 51 - 60 of 127
Scientific News
iCell® Neurons Enable Alzheimer’s Disease Modeling
Research demonstrate potential use of iCell® Neurons in high throughput screening at GlaxoSmithKline.
Galapagos Discovers Novel Candidate Drug to Treat Breast Cancer
GLPG1790 has high efficacy against triple-negative breast cancer.
A Molecular-Modeling Toolbox Aimed at Bridging the Gap Between Medicinal Chemistry and Computational Sciences
Researchers from the University of Basel have designed a versatile single-click tools to assist medicinal chemists in performing two routine modeling tasks.
Chemists Find Help from Nature in Fighting Cancer
Study of several dozen compounds based on a fungal chemical shows potent anti-tumor activity.
Gallo Center Scientists Identify Potential New Mechanism for Treating Problem Drinking
Researchers identified a potential new approach for reducing problem drinking: a new family of drugs with the ability to manipulate DNA structure without changing it.
€9m EU-project on Deep-Sea Organisms Started
The PharmaSea project will evaluate the potential of new bioactive compounds from marine organisms as novel drug leads or ingredients for nutrition or cosmetic applications.
Anti-cancer Drug Discovery and Development: Bcl-2 Family Small Molecule Inhibitors
In this article, researchers from The Pennsylvania University College of Medicine discuss the current status of Bcl-2 family small molecule inhibitors in preclinical and clinical development.
Chemists Devise Inexpensive, Benchtop Method for Marking and Selecting Cells
Chemists at The Scripps Research Institute have found an easier way to perform one of the most fundamental tasks in molecular biology.
Two MIT Professors Win Prestigious Wolf Prize
Michael Artin and Robert Langer honored for groundbreaking work in mathematics and chemistry.
Study Paves way to Design Drugs Aimed at Multiple Protein Targets at Once
Pharmaceutical chemists had suggested that the objective of a drug hitting multiple targets simultaneously is impossible and unlikely to succeed. This study shows how to efficiently and effectively make designer drugs that can do that.
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