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Ensuring the Quality of Registered Compounds in a Drug Discovery Environment – A Multidisciplinary Approach
Ryan Sasaki and Tara Sinclair

Lexicon Pharmaceuticals have demonstrated that a practical automated verification system using HPLC, LC/MS, and 1D and 2D NMR can be implemented in an industrial/pharmaceutical environment. This system has proven to be robust, and provides added value to compound collection integrity and quality.

Synthesis and Biological Evaluation of Novel Quinol dimethyl ethers as Potential Anticancer and Antimicrobial Agents
Ibrahim Chaaban, El Sayeda M. El Khawass, Mona A. Mahran, Heba A. Abd El Razik1, Nehad S. El Salamouni, Abeer E. Abdel Wahab

As a part of an ongoing research program devoted to the finding of new structural leads with potential chemotherapeutic activities, particular attention has been given to the pronounced anticancer activity of several quinol dimethyl ethers. Several analogs incorporating the above-mentioned quinol dimethyl ether counterpart together with a pyrazole moiety exhibited a potential antitumor activity.

The use of the IV microtracer technique to drive formulation optimisation
Vanessa Zann, Paul Dickinson, Wang Wang Lee, George Kirk, Owen Jones, Andy Gray, Davindera Singh Sanghera, Mark Seymour, Jo Collier, Lloyd Stevens, Julie Dent

Strategy: Use IV microtracer techniquer to de risk compounds with PK issues and drive formulation development

Addressing the challenges of poor solubility: Rapid development and clinical evaluation of a lipid based formulation to enhance oral bioavailability of amuvatinib (MP-470)
P.D. Scholes, J. McDermott, J. Vertommen, J-L Colin, G Choy, M Azab, R Joshi and S. Redkar

Physiochemical and biopharmaceutical properties of new chemical entities are presenting increasing challenges to successful oral drug delivery. Here we present data on amuvatinib, a novel multi-targeted tyrosine kinase inhibitor specifically designed to be a potent inhibitor of mutant c-Kit and PDGFRalpha.

Elucidation of the Relative Bioavailability of a Drug Candidate from Different Regions of the Human Gastrointestinal Tract
David Harris, Ph.d. , Joanne Collier, MBCHB, Alyson Connor, Ph. D. , Tomoko Freshwater, Ph. D. , David Goldfarb, Ph. D. , Ann Horowitsz Ph. D. , Xuewen Ma, Ph. D. , Paul Statkevich, Ph. D.

This poster describes a pharmacokinetic study to investigate the relative absorption of an NCE from different regions of the human gastrointestinal tract, to support potential development of a sustained-release formulation.

Evaluation Of Single Point And IC50 Shift Assays For Measuring Time-Dependent Inhibition Of Drug Discovery Compounds
Katie Fox, Rosey Pearson, Phillip Butler, Clive Dilworth

The aim of this study is to evaluate different assay designs, and data analysis methodology for measuring the extent of TDI for known inhibitors. We propose a reversible inhibition and TDI screening platform to cover early phase compounds, which enables accurate decisions to be made regarding development of compounds which could cause DDIs.

Nitric Oxide Decreases the Expression and Activity of the Ubiquitin-Conjugating Enzyme UbcH10
Nick D. Tsihlis, PhD, Chris S. Oustwani, BA, Ashley K. Vavra, MD, Qun Jiang, MD and Melina R. Kibbe, MD

Nitric oxide (NO) has been shown to limit the formation of neointimal hyperplasia in animal models of arterial injury. Ubiquitination proceeds via formation of thioester bonds and NO can act to disrupt those bonds. We report that NO decreases the activity and expression of UbcH10 in vitro, and decreases the expression of UbcH10 following arterial injury in vivo. Therefore, UbcH10 may be a promising therapeutic target for inhibiting neointimal hyperplasia.

SuperNatural: A Database of Available Natural Compounds
Melanie Füllbeck, Mathias Dunkel and Robert Preissner

The majority of marketed drugs are natural compounds or derivatives thereof. The compounds availability is often unclear. Therefore we have compiled a database of ~50,000 natural compounds. Starting point for in silico screenings are about 2,500 well-known, classified natural compounds or imported molecules. Possible medical applications can be detected and about three million conformers computed to account for the flexibility during usage of the 3D-superposition algorithm.

Microwave chemistry in SiC Reaction Vials
D. Obermayer, B. Gutmann, B. Reichart, C. O. Kappe

Using novel SiC-technology to mimic conventional heated autoclave experiments.

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Showing Results 71 - 80 of 174
Scientific News
UGA Researchers Discover Potential Treatment for Drug-resistant Tuberculosis
Researchers have developed a new small molecule drug as a treatment against multi-drug resistant tuberculosis.
A Protein's Novel Role In Several Types Of Cancers Discovered
Stanford ChEM-H scientists are helping to develop a novel cancer therapy based on a new finding of a protein that inadvertently promotes cancer growth.
Cancer Treatment with KU Origins Enters Second Clinical Trial
Cleave Biosciences has begun a Phase 1 clinical trial to evaluate CB-5083.
Grant will Help Develop More Powerful Disinfectants
$200,000 grant awarded to develop the next generation of antibacterial cleansers and disinfectants.
Artificially-intelligent Robot Scientist ‘Eve’ Could Boost Search for New Drugs
Eve, an artificially-intelligent ‘robot scientist’ could make drug discovery faster and much cheaper, say researchers writing in the Royal Society journal Interface.
Novogen Announces Important Discovery in Regenerative Medicine Program
A key proof-of-concept step to develop drugs capable of stimulating the function of brain tissue stem cells.
Stanford Chemists Take Step Toward Solving Mystery of How Enzymes Work
Steven Boxer and his students have found that the electrostatic field within an enzyme accounts for the lion's share of its success.
New Class of Synthetic Molecules Mimics Antibodies
A Yale University lab has crafted the first synthetic molecules that have both the targeting and response functions of antibodies.
The Hunt for Botanicals
Herbal medicine can be a double-edged sword and should be more rigorously investigated for both its beneficial and harmful effects, say researchers writing in a special supplement of Science.
Novel Agent Decreases Neuropathic Pain in Patients with Type 2 Diabetes
Promising profile of disease modification and pain reduction leads to proof of concept trials.
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