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Agenda
The MedChem Europe sessions will be held in parallel to the two tracks of Screening Europe and ADMET Europe sessions: Sessions Overview
Day 1 – February 19
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8:30 |
Registration
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9:30 |
Platforms and Combinatorial Chemistry
Aaron Beeler, Assistant Director, Centre for Chemical Methodology
and Library Development, Boston University
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9:35 |
New Approaches to the Discovery of Novel Chemical
Reactions and Chemotypes
Aaron Beeler, Assistant Director, Centre for Chemical Methodology
and Library Development, Boston University
Multidimensional reaction screening allows evaluation of chemical
reactions using multiple variables in a single array. Reactions may
be subsequently profiled through analytical techniques followed
by structure elucidation to identify new chemotypes and reaction
processes. Applications will be reviewed.
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10:05 |
New Organocatalytic Systems for Asymmetric Epoxidation
Phil Page, Professor of Organic Chemistry, University of East Anglia
Highly enantioselective iminium salt catalysts have been tested in the catalytic asymmetric epoxidation of unfunctionalized alkenes, giving up to 97% ee. Catalyst loadings as low as 0.1 mol% may be used.
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10:35 |
Coffee break and networking in exhibition hall
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11:20 |
Efficient Assembly and Selection of Macrocycle Libraries by
DNA-Programmed Chemistry
Jinbo Lee, Head of Chemistry, Ensemble Discovery Corporation
A large and structurally diverse macrocycle library using patented
DNA-programmed chemistry was prepared. Each library member is
linked to a unique DNA-tag that has directed its synthesis and also enables a powerful affinity-based selection process against important drug discovery targets.
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11:50 |
ConGO: A New Paradigm for Pattern Recognition of Drug
Electronic Structure
Maria Grishina, Associate Professor, Chelyabinsk State University
The combination of BiS/MC and ConGO algorithms (see modelchem.ru) is suggested for pattern recognition. BiS/MC obtains a drug conformer interacting with a receptor. ConGO analyses distribution of electron density. The approach recognition quality equals 1.0 for considered drug sets.
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12:20 |
Lunch & networking in exhibition hall
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12:50 |
 GE Healthcare Workshop: Applications of Microcarrier Cultured Cryopreserved Cells in Screening Assays for GPCRs
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13:20 |
Poster viewing
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14:00 |
High Throughput Synthetic Chemistry
Chaired by Thomas Müller, Professor, Chair of Organic Chemistry, Heinrich-Heine-University Düsseldorf
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14:05 |
Synthesis of Pharmacologically Relevant Ring Systems by
One-Pot Cyclizations
Peter Langer, Professor, Institute for Chemistry, Department of
Organic Chemistry, University of Rostock
Catalytic one-pot cyclization reactions were developed.
These transformations allow an efficient synthesis of various
pharmacologically relevant ring systems.
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14:35 |
Applications of Multicomponent Reactions (MCRs) in Library Synthesis
János Gerencsér, Assistant Director, Chemistry and Innovation, AMRI
Novel applications of Biginelli and Yonemitsu reactions in different library synthesis programs will be discussed.
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15:05 |
Coffee break and networking in exhibition hall
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16:20 |
Multi-Component and Domino Syntheses of Pharmaceutically
Relevant Heterocycles
Thomas Müller, Professor, Chair of Organic Chemistry, Heinrich-
Heine-University Düsseldorf
Coupling-isomerization and coupling-addition reactions, in combination with condensation chemistry, are new, straightforward entries to diversity-oriented multi-component and domino syntheses of pharmacologically relevant heterocycles and complex structural scaffolds in a one-pot fashion.
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16:50 |
Dihydropyridine Derivatives and Dihydroazines as
Bioprotectors
Gunars Duburs, Professor, Latvian Institute of Organic Synthesis
1,4-Dihydropyridines possess electron/hydrogen donor, peptide type and lipid like character, reveal bioprotective properties: radioprotective, antimutagenic, life span prolongation, neuroprotective, memory enhancing, antidiabetic, antiinflammation, antiischaemic, antihypertensive, antianginal, gene transfection activities. Green chemistry approach and chemoenzymatic transformations have been used .
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17:20 |
Drinks reception compliments of HTScreening.net |
Day 2 – February 20
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8:00 |
 TTP Labtech Workshop: Achieving Acurate Nanolitre Pipetting for Miniaturising Serial Dilutions and Assay-Ready Plates
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Target Identification and Lead Optimisation
Co-Chaired by Andreas Sewing, Research Fellow/Director, Pfizer and Dmitry Samarsky, VP, Technology Development, RXi Pharmaceuticals
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| 9:35 |
Time Dependent Cytochrome P450 Inhibition: Review of
the Common Sub-Structures and Implications for Drug
Development
Patrick Dansette, Research Director and head of the Cytochrome P450 team, CNRS UMR8601
Time dependent inhibition of cytochrome P450 can lead to serious
consequences (DDI) in patients. There are screening tools today
which can identify very early TDI inhibitors and medicinal chemistry programs should integrate them early in the drug discovery process.
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| 10:05 |
Molecular Effects of Akt and Src on the Activity of mTOR-Dependent Signalling Pathway in v-Src-Transformed Cells
Zdena Tuhackova, Senior Researcher, Institute of Molecular Genetics, Academy of Sciences of Czech Republic
Regulation of the mTOR signalling pathway by Src implies that not
only rapamycin and its analogs that are potential antitumour agents, also inhibitors of Src kinase activity may display therapeutical effect in tumours in which mTOR signalling pathway is activated.
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10:35 |
Coffee break and networking in exhibition hall
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11:20 |
Analogs of Griseofulvin with Enhanced Anticancer Activity
Mads Clausen, Assistant Professor, Technical University of Denmark
Griseofulvin induces mitotic arrest and apoptosis in a mechanism
very selective to cancer cells. The group has synthesized analogs of griseofulvin to obtain SAR data and has significantly improved the activity compared to the natural product.
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| 11:50 |
Improving Processes in Lead Optimisation
Andreas Sewing, Research Fellow/Director, Pfizer
Already successfully applied across different industries, lean and 6
sigma related tools can be applied to pharmaceutical R&D to increase business excellence and drive efficiency of the Hit to CAN process. This will be illustrated with examples from the work of Pfizer.
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| 12:20 |
Lunch & networking in exhibition hall
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13:00 |
Poster viewing
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| 13:30 |
Development and Optimization of Novel RNAi Therapeutics
Platforms
Dmitry Samarsky, VP, Technology Development, RXi Pharmaceuticals
The design of therapeutic RNAi triggers will be discussed. Also,
nanotransporter delivery of RNAi compounds to mouse tissues will
be illustrated and silencing of SOD1 in an ALS model demonstrated. Lastly, validation of RIP140 as a target for obesity will be described.
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| 14:00 |
Coffee break and networking
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14:30 |
Structure Based Design of a Novel and Highly Potent Anti-HIV
Non-Nucleosidic-Reverse-Transcriptase-Inhibitor: IDX12899
Christophe Parsy, Associate Director, Idenix Pharmaceuticals
HIV-therapy multidrug regimens require the development of new drugs with better resistance profile to overcome the emergence of mutants. Efforts to discover new NNRTI led to the discovery of IDX12899, a highly potent inhibitor of the HIV-1 Reverse Transcriptase.
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| 15:00 |
HDAC Inhibitors: Bench to Bedside
Thomas Miller, Senior Research Fellow, Merck Research Laboratories
The discovery and development of Zolinza™ (SAHA, vorinostat), a novel hydroxamic acid derived HDAC inhibitor, along with relevant background and recent advances in HDAC inhibitor design, will be presented.
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| 15:30 |
Close of conference |
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