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Natural Products Targeting Oncology Pathways
04 May 2010: In this application note, BioFocus present three examples for natural compounds targeting specific tumor pathways: geldanamycin, borrelidin and fredericamycin. Gram quantities of the compounds are generated using microbial producers and semi-synthesis subsequently generates focused libraries of natural compound analogs. In vivo and in vitro protocols are then used to test potential anticancer properties of the compounds.
BioFocus
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Epigenetics Targets –Efficient Hit-Finding Approaches
04 May 2010: In this application note BioFocus use epigenetic targets to identify starting points for lead optimizaton. In order to address a broad range of novel epigenetics targets, rather than screening a full compound collection, BioFocus use computational chemistry workflows which are individually tailored and optimized for selecting the most suited compounds from library subsets for primary screening. These filtered high-throughput screens generate a greatly increased hit-rate.
BioFocus
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Are Natural Products Delivering? Experiences and Recommendations from 27 Screening Campaigns
04 May 2010: In this application note from BioFocus, microbial strain subfractions are generated and used in high-throughput screens (HTS) for analysis with regard to diversity, selectivity and strain origin. Natural compounds were identified during the follow up of subfraction screening programs and their chemical properties have been analyzed. Searches in natural product databases revealed that 135 of the 645 identified natural compounds are novel compounds.
BioFocus
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FastLC Application Curcumin
22 Apr 2009: The plant pigment curcumin found in turmeric is highly active against the growth of certain cancers. Therefore researches have high expectations that curcumin can be administered as phytotherapeutic drug in order to prevent metastasis. YMC has developed a method which enables analysis of curcumin and related polyphenolic compounds in less than 3 minutes. It is based on YMC-UltraHT ProC18, a 2μm packing material specifically designed for FastLC.
YMC Europe GmbH
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Achiral Stationary Phase Selectivity under Supercritical Fluid Chromatography (SFC) Conditions
02 Dec 2008: Supercritical fluid chromatography (SFC) is gaining wide acceptance in the pharmaceutical industry in support of drug discovery and medicinal chemistry compound separation and purification. Until recently SFC has found the greatest success in small preparative scale chiral separations in drug discovery laboratories. However, this application notes demonstrates that there is significant potential for extending SFC to achiral column screening and method development.
Phenomenex Inc
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Alternative Selectivity of Chiral Stationary Phases Based on Cellulose tris(3-chloro-4-methylphenylcarbamate) and Cellulose tris(3,5-dimethylphenylcarbamate)
02 Dec 2008: Polysaccharide-based chiral stationary phases (CSP) are widely used due to their wide chiral recognition ability. This application note demonstrates the different chiral recognition capabilities of CSPs. Numerous examples including important classes of drug compounds as well as statistical data prove that cellulose tris(3-chloro-4 methylphenylcarbamate) offers a good alternative to the commonly used cellulose tris(3,5- dimethylphenylcarbamate) in the separation of difficult racemic mixtures.
Phenomenex Inc
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Structural Optimization of Leads to Improve ADME Properties
 30 Apr 2008: One of the most challenging problems during the lead optimization phase of a potential drug candidate is achieving the right balance between efficacy, patentability concerns, toxicity, and ADME properties. This application note discusses how ACD/Labs’ Structure Designer software can be used to propose structural modifications of lead compounds to improve physicochemical properties such as logP and solubility.
Advanced Chemistry Development, Inc., (ACD/Labs)
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Assembling Fragment Libraries
 22 Apr 2008: One of the key considerations when designing and assembling fragment libraries is the type of the screening platform that will be used to detect the interaction between the biological target and the fragment. This poster demonstrates the construction of two libraries of fragments. One library has been built for use in high-throughput biochemical screening assays and the other was purposefully designed for screening using NMR techniques.
Evotec technologies
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Novel Bcl-2 family inhibitors by fragment and virtual screening
22 Apr 2008: This poster demonstrates that by using the EVOlution™ platform for fragment-based drug discovery (FBDD) and structure-based drug design, we have discovered by fragment and virtual screening, novel inhibitors of Bcl-2, Bcl-xL and Mcl-1. This has afforded to date four series of drug-like Bcl-2 family inhibitors with multiple actives in the micromolar range and several singleton hits.
Evotec technologies
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