ASMC'13 Moscow

Synthetic Organic Photochemistry in Batch and Flow

Prof. Kevin BOOKER-MILBURN

UNIVERSITY OF BRISTOL, Bristol, United Kingdom
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Prof. Kevin BOOKER-MILBURN

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Our research is concerned with the generation of new synthetic methods for the construction of complex organic molecules. Methods include the use of photochemistry and new Pd(II) catalysed methods that involve C-H activation pathways. Our synthetic targets include biologically active complex polycyclic alkaloids and terpenes. Kevin Booker-Milburn received his BSc Hons from Paisley College of Technology in 1985 and his Glaxo funded PhD in synthetic organic chemistry from the University of Strathclyde in 1988. After a period of postdoctoral work with Professor Phillip J. Parsons at the Universities of Southampton and Reading he obtained a Lectureship at the University of Salford in 1991. In 1994 he moved to the University of East Anglia where he was promoted to Reader in 1997. He then moved to the University of Bristol in 1999 and was promoted to Professor in 2006. He has recieved the Glaxo-Welcome award for Organic Chemistry, the AstraZeneca award for Organic Synthesis and the RSC Bader Award. Professor Booker-Milburn is currently the Director of the EPSRC Doctoral Training Centre in Chemical Synthesis based at Bristol.

Making Molecular Prosthetics via Iterative Cross-Coupling with MIDA Boronates

Prof. Martin D. BURKE

UNIVERSITY OF ILLINOIS, Urbana, United States
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Prof. Martin D. BURKE

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Marty Burke completed his undergraduate studies in chemistry at Johns Hopkins University in 1998. He then moved to Harvard Medical School and MIT as a PhD/MD student in the interdisciplinary Health Sciences and Technology program. From 1999-2003 he completed his thesis research as an HHMI Graduate Fellow under the direction of Professor Stuart Schreiber at Harvard University. After finishing his clinical rotations as an NIH Fellow in the Medical Scientist Training Program, he graduated from medical school in 2005. That same year Marty joined the Department of Chemistry at the University of Illinois at Urbana-Champaign as an Assistant Professor of Chemistry. In 2009 his lab was selected to join Howard Hughes Medical Institute, and in 2011 he was promoted to Associate Professor. Research in the Burke group focuses on the synthesis and study of small molecules that perform protein-like functions. These efforts seek to build the foundation for the development of molecular prosthetics as a general strategy for the betterment of human health. To enable these studies, Marty's group is pioneering a synthesis strategy, dubbed iterative cross-coupling, that aims to make the process of complex small molecule synthesis as simple, efficient, and flexible as possible. This work has led to the development of more than 125 commercially-available MIDA boronate building blocks that are enabling the more effective synthesis of small molecules in many academic and industrial institutions throughout the world, including applications on the process scale to support clinical studies in humans. Marty's group is now harnessing the power of this chemistry to understand the protein-like activities of a variety of prototypical small molecule natural products, including the ion channel-forming polyene macrolide amphotericin B and the antilipoperoxidant carotenoid peridinin. Marty is the recipient of a number of honors and awards, including the American Chemical Society’s Arthur C. Cope Scholar Award, a Howard Hughes Medical Institute Early Career Scientist Award, a Sloan Foundation Research Fellowship, the Arnold and Mabel Beckman Foundation Young Investigator Award, an NSF CAREER award, the Dreyfus Foundation New Faculty Award, the Bristol-Myers Squibb Unrestricted Research Grant in Synthetic Organic Chemistry, the Eli Lilly Grantee Award, the Amgen Young Investigator Award, the AstraZeneca Excellence in Chemistry Award, and he has been named “one of the world's 35 top innovators under age 35” by Technology Review. He has also been extensively recognized for excellence in teaching at both the undergraduate and graduate levels.

Oligonucleotide Synthesis Interfaced with Molecular Biology and Nanotechnology

Prof. Marvin CARUTHERS

UNIVERSITY OF COLORADO, Boulder, United States
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Prof. Marvin CARUTHERS

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Title and Position: Distinguished Professor, Department of Chemistry and Biochemistry, University of Colorado
Research Field: The Caruthers laboratory focuses primarily on the chemical synthesis of DNA, RNA and their analogues. Applications in biology and nanomaterials for these new analogues are then investigated.
Education: B. S. from the Department of Chemistry, Iowa State University, Ames, Iowa. Ph. D from the Department of Chemistry and Biochemistry, Northwestern University, Evanston, Illinois.

BETting on Epigenetic Targets : From Phenotypic Discovery to First Time in Man

Dr Chun-wa CHUNG

GLAXOSMITHKLINE, Stevenage, United Kingdom
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Dr Chun-wa CHUNG

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Current title and position: Group Leader of Structural and Biophysical Analysis, Computational and Structural Chemistry, GlaxoSmithKline R&D, Stevenage, UK
Research field: Application of structural biology (NMR, Xray) and biophysical methods (SPR, ITC, MS) for mode of action, hit triage and hit identification including fragment based screening. Particular interest in field of epigenetic drug discovery.
Education and past experience: BA Natural Sciences (Chemistry), University of Cambridge. PHD in NMR techniques development with Dr James Keeler, University of Cambridge.

Versatile Synthetic Methods: Access to Bioactive Molecules

Prof. Janine COSSY

ESPCI PARISTECH, Paris, France
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Prof. Janine COSSY

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http://www.lco.espci.fr/_private/Pages_perso/Janine%20Cossy/janine_cossy.htm

Current Position
Professor of Organic Chemistry, ESPCI ParisTeh, Paris, France

Research field
Photochemistry, thermal reactions, radicals, rearrangements, enantioselectivity, organometallic chemistry, catalysis, synthesis of natural products and/or biologically active compounds.

Education and former Professional Experience
1974: Master, University of Champagne-Ardenne at Reims, France
1979: Ph.D., University of Champagne-Ardenne at Reims, France (Supervisor: Pr J. P. Pète)
1980-1982 Postdoctoral Fellow, University of Wisconsin, Madison (USA) (Supervisor Pr B. M. Trost)
1976-1990 CNRS Research Assistant, University of Champagne-Ardenne at Reims, France
Oct 1990 CNRS Director of Research, University of Champagne-Ardenne at Reims, France
Since Nov 1990 Professor of Organic Chemistry, ESPCI ParisTeh, Paris, France

Identification of a Novel Series of Orexin Receptor Antagonists with a Distinct Effect on Sleep Architecture

Dr Simona COTESTA

NOVARTIS, Basel, Switzerland
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Dr Simona COTESTA

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Investigator III, Novartis Institute for Biomedical Research (NIBR), Computer Aided Drug Discovery. PhD in Biochemistry, ETH Zürich (Switzerland). Post-Doctoral position in computational chemistry and cheminformatics at Roche AG (Basel, Switzerland)

Highly Anti-inflammatory Dendritic Polyglycerol Sulfates - a Multiple Target Approach

Prof. Rainer HAAG

FREE UNIVERSITY BERLIN, Berlin, Germany
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Prof. Rainer HAAG

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Rainer Haag, born 1968, is Full Professor in Organic and Macromolecular Chemistry at the Freie Universität Berlin. Since 2008 he is the head of a collaborative research center SFB 765 “Multivalency a chemical organization and action principle”. His research interests are dendritic polymers as highly functional polymeric supports for catalysis, macromolecular nanotransporters for DNA- and drug-delivery and protein resistant material surfaces. In 2004 his group was awarded the young investigator NanoFutur award from the German Ministry of Science (BMBF) and in 2010 the Athur K. Doolittle Award of the American Chemical Society (ACS) for their work on “multifunctional nanotransport systems”. He is also advisor for two start-up companies (mivenion and nanopartica) that license the group’s technology.

Targeting Protein Surfaces Using Designed Proteomimetics

Prof. Andrew HAMILTON

UNIVERSITY OF OXFORD, Oxford, United Kingdom
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Prof. Andrew HAMILTON

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Professor Andrew Hamilton, Vice-Chancellor of Oxford University since October 2009. Read chemistry at Exeter University, Masters from University of British Columbia and PhD from Cambridge. Joined Yale in 1997, Provost 2004-2008, combining administrative duties, teaching and research. Research focuses on use of synthetic design for understanding, mimicry and potential disruption of biological processes. Fellow Royal Society and Member American Academy of Arts & Sciences. Received the International Izatt Christiansen Award in Macrocyclic Chemistry in 2011.

A New Approach to Tuberculosis Research: The Lilly TB Drug Discovery Initiative

Dr Philip A. HIPSKIND

ELI LILLY & COMPANY, Indianapolis, United States
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Dr Philip A. HIPSKIND

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Philip A. Hipskind, Ph.D. , currently a Distinguished Research Fellow within Lilly Research Laboratories, earned his B.S. degree from Indiana University, Bloomington conducting undergraduate research with Professor Paul Grieco and his doctorate in synthetic organic chemistry with Professor Barry Trost at Stanford University in 1991. Since 1991, he has worked at Lilly in the Anti-Infective, Neuroscience, Endocrinology, and Oncology therapeutic areas. While currently pursuing novel treatment modalities in oncology, Dr. Hipskind also leads the Lilly Tuberculosis Drug Discovery Initiative – a not for profit, public – private research enterprise.

Design and Optimization of Pyrazinecarboxamide-Based Inhibitors of Diacylglycerol Acyltransferase 1 (DGAT1) Leading to the Clinical Candidate AZD7687

Dr Petra JOHANNESSON

ASTRAZENECA, Mölndal, Sweden
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Dr Petra JOHANNESSON

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Petra obtained her Master of Science in Pharmacy and PhD in Organic Pharmaceutical Chemistry at Uppsala university, Sweden. After working a couple of years in small biotech, she joined AstraZeneca R&D Mölndal, Sweden in 2004 as a synthetic and medicinal chemist, where she has been involved in various projects within the cardiovascular and metabolic disease areas. She currently holds a position as team leader in Medicinal Chemistry at the Cardiovascular and Gastrointestinal Innovative Medicines Unit at AstraZeneca R&D Mölndal, Sweden.

Harnessing Synergy Between Natural Products and Synthesis Towards Drug Discovery

Prof. Goverdhan MEHTA

UNIVERSITY OF HYDERABAD, Hyderabad, India
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Prof. Goverdhan MEHTA

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Goverdhan Mehta is currently National Research Professor and Jubilant-Bhartia Chair at the University of Hyderabad. He has held positions at the Indian Institute of Science and the University of Hyderabad, two premier institutions in India, as the Director and Vice chancellor, respectively. He is a recipient of numerous awards and medals including some from the Indian Chemical Society, Royal Society of Chemistry, UK. And TWAS, Trieste, Italy. He is a Fellow of several Science academies including the Royal Society (FRS) of UK and is a Foreign Member of the Russian Academy of Sciences. He is also an Honorary Fellow (HonFRSC) of the Royal Society of Chemistry, UK. His research interests are mainly in contemporary organic synthesis and he has published and lectured extensively.

New Strategies in Organic Synthesis: Recent Advances Based on Catalytic Reactions of Boron Reagents

Prof. James P. MORKEN

BOSTON COLLEGE, Chestnut Hill, United States
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Prof. James P. MORKEN

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James P. Morken is a Professor of Chemistry at Boston College. He obtained his B.S. in chemistry in 1989 from UC Santa Barbara working with Bruce Rickborn, and a Ph.D. from Boston College in 1995 with Amir Hoveyda. He was an NSF Postdoctoral Fellow with Stuart Schreiber at Harvard University and, in 1997, became an Assistant Professor at the University of North Carolina at Chapel Hill. He was promoted to Associate Professor in 2002 and in 2006 joined the faculty of Boston College as a Professor of Chemistry. His research focuses on the development of transition-metal-catalyzed asymmetric processes and their use in complex molecule synthesis.

P2X Receptors: ATP-Gated Ion Channels as Novel Drug Targets

Prof. Christa MÜLLER

UNIVERSITY OF BONN, Bonn, Germany
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Prof. Christa MÜLLER

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Head of Pharmaceutical Chemistry I, Pharmaceutical Institute
http://mueller-group.pharma.uni-bonn.de
Research field: Medicinal chemistry of purine-binding membrane proteins (P2, adenosine, adenine receptors, and ecto-nucleotidases); lipid-activated GPCRs, orphan GPCRs
- 1988: Ph.D. (Dr. rer. nat.), University of Tübingen
- 1989/90 and 1992: Postdoctoral scientist at NIH, USA
- 1994-1998: Associate Professor (C3) University of Würzburg
- since 1998: Full Professor (C4) University of Bonn, Germany
- 2001-2004: Vice-rector for planning and finances at the University of Bonn
- since 2011: Elected spokesperson of the PharmaCenter Bonn
- since 2010: Vice-rector for public and international relations, Univ. Bonn
- since 2008: Member of the selection committee of the Humboldt (AvH) Foundation
- 2010: PHOENIX Pharmazie Science Prize (Pharmaceutical Chemistry)
- 2011: Research Prize of Alzheimer Forschung Initiative e.V.
- 2013: Prize for Inventors by the Ministery of North-Rhine Westfalia

Advances in Targeting Voltage-Gated Sodium Channels with Small Molecules

Dr Antonio NARDI

GRÜNENTHAL, Aachen, Germany
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Dr Antonio NARDI

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Dr. Antonio Nardi holds a PhD in medicinal chemistry (2004) awarded from Pisa University and carried out both at Department of Pharmaceutical Sciences (Pisa, Italy) and Hoffmann-La Roche AG Laboratories, Discovery Chemistry (Basel, Switzerland). After his PhD, he obtained first a post-doc (2005-2006) and later (2006-2010) a position as a research chemist and project leader at NeuroSearch A/S (Ballerup, Denmark), a biopharmaceutical company focused on ion channel modulators for the treatment of unmet medical needs, mainly within the CNS. In 2010, Dr. Nardi has joined the Medicinal Chemistry department of the Global Drug Discovery division at Grünenthal (www.grunenthal.com) in Aachen (Germany) as Associate Scientific Director. Since then he has been involved and led research programmes aimed at a finding novel small molecules for treating inflammation and pain.

Organic Molecules as Biological Probes...an exciting journey

Prof. Cristina NEVADO

UNIVERSITY OF ZURICH, Zurich, Switzerland
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Prof. Cristina NEVADO

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Cristina Nevado was born in 1977 in Madrid, where she graduated in chemistry at the Autónoma University in 2000. In October 2004 she received her PhD in organic chemisty at the same university working with Prof. Antonio M. Echavarren in the cyclization of enynes catalyzed by platinum and gold complexes. In December 2006 she joined the group of Prof. Alois Fürstner at the Max-Planck-Institut für Kohlenforschung (Germany) where she was part of the team who conquered the first total synthesis of Iejimalide B, a marine macrolide possesing a very sensitive architecture. In May 2007 she started her independent career as an Assistant Professor at the University of Zürich. In 2011, Cristina was awarded the Chemical Society Reviews Emerging Investigator Award and the Thieme Chemistry Journal Award in recognition of her contributions in the field of synthetic organic chemistry. In 2012 she received an ERC Junior Investigator grant and has been awarded the Werner Prize of the Swiss Chemical Society. In 2013 she become Full Professor at the Organic Chemistry Institute of the University of Zürich. Rooted in the wide area of organic chemistry, her research program is focused on complex chemical synthesis and new organometallic reactions.

Bitopertin (RG1678), a Potent and Selective Glycine Re-Uptake Inhibitor for the Treatment of Schizophrenia

Dr Emmanuel PINARD

F. HOFFMANN-LA ROCHE, Basel, Switzerland
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Dr Emmanuel PINARD

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Career highlights:
- phD in Chemistry at the university of P. et M. Curie in Paris
- Post-doc in the group of Professor L. Paquette at the Ohio State University
- Joined in 1994 the Drug Discovery Chemistry unit of Hoffmann-La Roche, Basel as medicinal chemist. Since 2001, team leader in various projects targeting CNS targets. Currently leading the Roche Glyt1 discovery project.
- More than 60 patents and 30 publications

Antibody Drug Conjugates for the Treatment of Cancer

Dr Paul POLAKIS

GENENTECH, San Francisco, United States
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Dr Paul POLAKIS

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Currently a Staff Scientist and Director, Cancer Targets, Dept. of Research.
Areas of Interest:
1. Research and early development of antibody drug conjugates as cancer therapeutics.
2. Wnt signaling in Cancer.
Education: Ph.D., Biochemistry, Michigan State University 1984
Professional Experience: Post doc, Duke University/Scientist-Senior Scientist, Chiron Corporation/ Research Director, Onyx Pharmaceuticals/ Senior Scientist-Staff Scientist-Director, Genentech, Inc./Roche.

Peptide Chemologics

Dr Lee ROBERTS

PFIZER, Sandwich, United Kingdom
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Dr Lee ROBERTS

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Lee Roberts is an Associate Research Fellow within the Biotherapeutics chemistry group in Pfizer, Cambridge, USA supporting inflammation and rare diseases having recently transferred over from the Pfizer UK Sandwich Site. He has worked across a number of therapeutic areas and diverse classes of targets and on a number of modalities including small molecules, peptides, peptidomimetics, protein epitope mimetics, bioconjugates and antigens for therapeutic vaccines and monoclonal antibodies. He studied for his PhD under Professor William Motherwell at Imperial College before undertaking post-doctoral research at UCLA with Prof Mike Jung followed by further post-doctoral studies with Prof Gerry Pattenden at the University of Nottingham.

The Discovery of the Macrocyclic HCV NS3/4A Protease Inhibitor MK-5172

Dr Michael ROWLEY

MERCK RESEARCH LABORATORIES, Kriens, Switzerland
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Dr Michael ROWLEY

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Mike obtained his MA and PhD in Cambridge, UK followed by two years at Postdoc at Harvard in Cambridge, MA. In 1988 he joined MSD in the UK as a medicinal chemist, where he was involved in various neuroscience projects in the areas of cerebral ischemia, depression, anxiety, and pain. In 2000, Mike moved to become responsible for Medicinal Chemistry and DMPK at IRBM (Merck’s site in Rome), working in the areas of antivirals and cancer. It was during this time that the group in Rome, in close collaboration with other Merck scientists, discovered both Isentress™, the first in class inhibitor of HIV Integrase and MK-5172, an HCV protease inhibitor in Phase IIB. He joined AstraZeneca in Mölndal, Sweden in 2009 as Head of Medicinal Chemistry for the Cardiovascular and Gastrointestinal Research Area. He came back to MSD in his current position of Associate Scientific Vice President in MRL Global Chemistry in 2012.

The Design and Characterization of Targeted Covalent Inhibitors of Btk

Dr Eric SCHWARTZ

CELGENE AVILOMICS RESEARCH, Cambridge, United States
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Dr Eric SCHWARTZ

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Eric is currently Senior Director of Chemistry at Celgene Avilomics Research in Bedford, MA. He has worked in the area of small molecule drug discovery, mainly oncology and inflammation, since 1990 when he started his career at Eisai Research Institute. In 1999, he moved to UCB Research as a Principal Scientist, later becoming Assoc. Director and then Director of Medicinal Chemistry for the site in Cambridge, MA. Following a short stint at Biogen-Idec in 2005, Eric moved to the newly formed start-up Resolvyx Pharmaceuticals as Senior Director and then V.P. of Chemistry. In 2011, he moved to another start-up, Avila Therapeutics, which focused solely on targeted covalent inhibitors. Avila was acquired by Celgene in March 2012 and the site renamed as Celgene Avilomics Research. Eric received a B.S. from the Ohio State University (1983), a Ph.D. in organic chemistry with Prof. Ed Vedejs at the University of Wisconsin-Madison (1988) and followed that with a post-doctoral fellowship at the University of Pittsburgh under Prof. Dennis Curran.

From Organic Synthesis to Biomedical Sciences - from Polyhydroxybutyrate (PHB) to Cell-Penetrating Peptides

Prof. Dieter SEEBACH

ETH ZURICH, Zürich, Switzerland
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Prof. Dieter SEEBACH

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Dieter Seebach received his PhD from the Technische Hochschule Karlsruhe (now KIT) and was Professor of Chemistry at the Justus-Liebig Universität in Giessen (1971-1977) and at ETH Zürich, Switzerland (1977-2003), wher he is now Professor emeritus. His past and present research activities include: Development of New Synthetic methods (umpolung of reactivity, self-regeneration of chirality centers, the gem.-diaryl effect in stereoselective synthesis), Natural-product synthesis, Structure determination, Chiral dendrimers, The Biopolymer PHB, -Peptides, Medicinal Chemistry of Peptides.

Engineering of Small Non-Antibody Protein Scaffolds as Novel Biopharmaceuticals: from Anticalins to PASylation

Prof. Arne SKERRA

TECHNICAL UNIVERSITY MUNICH, München, Germany
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Prof. Arne SKERRA

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Dr Arne Skerra is Full Professor at the Technische Universitaet Muenchen, where he heads the Institute of Biological Chemistry. He holds a Diplom degree in Chemistry from the Technische Universitaet Darmstadt and a PhD in Biochemistry from the Ludwig-Maximilians-Universitaet Muenchen. After post-doctoral studies at the MRC Laboratory of Molecular Biology in Cambridge, UK, and a group leader position at the Max-Planck-Institute for Biophysics in Frankfurt am Main he became Associate Professor for Protein Chemistry at the TU Darmstadt. In 1998 he moved to the TU Munich, where he was appointed to the Chair of Biological Chemistry at the Life Science Campus Weihenstephan. Arne Skerra started his scientific career in the field of protein engineering, where he pioneered, together with Andreas Plueckthun, the biosynthesis of functional antibody fragments in E. coli. Since then, he made several important contributions to this area, including the development of the Strep-tag technology for the purification of recombinant proteins. Currently, his main field of research is the design and structural analysis of proteins. One focus is the functional engineering of lipocalin proteins, where he developed ‘Anticalins’ as a novel class of therapeutic proteins. In order to advance this technology to the clinical stage he founded in 2001 Pieris AG, a German biotech startup company. Lately, he also became interested in improving the pharmacological properties of therapeutic proteins, in particular plasma half-life, which led to the development of 'PASylation'. In 2009 he founded the biotech startup company XL-protein GmbH to further exploit this technology.

Metal Catalyzed Arylation of Nucleophiles

Dr Marc TAILLEFER

ENSCM, Montpellier, France
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Dr Marc TAILLEFER

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Marc Taillefer received his PhD (supervised by Igor Tkatchenko and Jean-Jacques Brunet) from the University Paul Sabatier, Toulouse, in 1990. After postdoctoral work with Wolfgang A. Herrmann at the Technische Universität München, he was recruited at CNRS and started his research at the École Nationale Supérieure de Chimie de Montpellier . He is currently CNRS Research Director and head of the research group on Molecular Synthesis Methodology at the Institut Charles Gerhardt Montpellier. In 2010, he received the Prix Clavel-Lespiau of the French Académie des Sciences, awarded every four years, for his work in organic synthesis. This year, he was the laureate of the ‘‘European Sustainable Chemistry Award 2012’’ attributed by EuCheMS. Marc Taillefer is chairman of the Organic Chemistry Division of the French Chemical Society (SCF), and vice-president of the SCF.

Discovery and Initial Clinical Results of [¹⁸F]-UCB-H, First PET Radiotracer Targeting Synaptic Vesicle 2A

Dr Anne VALADE

UCB, Braine-l'Alleud, Belgium
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Dr Anne VALADE

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Current title and position: Principal Scientist in Medicinal Chemistry, UCB Pharma, Braine l’Alleud, Belgium.
Research field: focus on central nervous system (CNS) disorders and immunology diseases to deliver more convenient and effective treatments for patients and specialists.
Education and past experience:
Postdoctoral Research Fellow with Prof. David Hodgson, University of Oxford, U.K. (2004-2006) - Synthetic Studies Towards Squalestatin
Ph.D. in Organic Chemistry with Prof. J.-M. Beau, Paris XI University (Orsay), France (2001-2004) - Selection of Glycosyltransferase Modulators by Dynamic Combinatorial Chemistry

EFMC Prize for a Young Medicinal Chemist in Academia
Chemical Approaches to Biology and Therapeutics

Prof. Gonçalo BERNARDES

INSTITUTO DE MEDICINA MOLECULAR, PORTUGAL & UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom
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Prof. Gonçalo BERNARDES

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https://www.ch.cam.ac.uk/person/gb453

Gonçalo graduated in Chemistry from the University of Lisbon in 2004. He then moved to the University of Oxford where he completed his D.Phil. degree in 2008 under the supervision of Prof. Ben Davis working on reaction engineering for site-selective protein modification. He was awarded a Marie-Curie Fellowship to perform postdoctoral studies with Prof. Peter H. Seeberger, after which he returned to Portugal to work as a Group Leader at Alfama Inc., a spin-out company dedicated to the development of Carbon Monoxide-Releasing Molecules (CO-RMs). From September 2010 until October 2012, Gonçalo was an EMBO and Novartis Research Fellow in the group of Prof. Dario Neri at the ETH Zürich where he developed novel vascular targeting antibody-drug conjugates (ADCs) for cancer therapy. Gonçalo has been recently awarded a prestigious Royal Society University Research Fellowship, UK to start his independent research career at the University of Cambridge, UK. He is also the new Director of the Chemical Biology and Pharmaceutical Biotechnology Unit at the Instituto de Medicina Molecular in Lisbon. His research has resulted in more than 30 peer review publications with an h-index of 11, 4 patents and he has been invited to present his research in more than 50 conferences/institutes worldwide.

EFMC Prize for a Young Medicinal Chemist in Industry
Free-Wilson and Structural Approaches to Co-Optimising Human and Rodent Isoform Potency for 11β-Hydroxysteroid Dehydrogenase Type 1 (11β -HSD1) Inhibitors

Dr Frederick W. GOLDBERG

ASTRAZENECA, Macclesfield, United Kingdom
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Dr Frederick W. GOLDBERG

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Frederick Goldberg received his masters from Cambridge University in 2000 and his PhD at Imperial College London in 2004, then received a Fulbright scholarship to perform postdoctoral studies with Philip Magnus at the University of Texas at Austin. He returned to the UK in 2006 to work for AstraZeneca as a medicinal chemist, initially as associate team leader, then team leader and now senior medicinal chemist. He has worked across all discovery phases in diabetes and oncology disease areas, and his research interests include kinases, structure based design, compound collection enhancement, chemical biology and metabolism

Novel Synthetic Chemical Chaperones as a New Basis For Amyotrophic Lateral Sclerosis (ALS) Treatment

Prof. Arie-Lev GRUZMAN

BAR ILAN UNIVERSITY, Ramat Gan, Israel
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Prof. Arie-Lev GRUZMAN

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Senior Lecturer (Assistant Professor), Vice-president of The Medicinal Chemistry Section of the Israel Chemical Society, Division of Medicinal Chemistry, Department of Chemistry, Faculty of Exact Science, Bar Ilan University, Ramat Gan, Israel. Development of new drugs against diabetes type two, prostate cancer, Amyotrophic Lateral Sclerosis (ALS), catecholamine induced arrhythmia and autoimmune diseases. 1993 - 1995: B.Sc., Chemistry Bar Ilan University, Ramat Gan, Israel. 1997 - 2003: Ph.D (Summa cum Laude), Medicinal Chemistry and Pharmacology, School of Pharmacy, Faculty of Medicine, Hebrew University of Jerusalem, Israel. 2004 - 2007: Post-Doctoral Research Fellow, Biochemistry Department of Physiology, Medical School, University of California, San Francisco and Research Institute of Pacific Medical Center at San Francisco, U.S.A. Supervisor: Prof. Vishvanath Lingappa.

New Inhibitors of the Enzyme Isoprenylcysteine Carboxyl Methyltransferase (ICMT)

Prof. Maria del Mar MARTIN-FONTECHA

COMPLUTENSE UNIVERSITY OF MADRID, Madrid, Spain
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Prof. Maria del Mar MARTIN-FONTECHA

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Current position
Assistant Professor from 2009 to present (Organic Chemistry Department, Complutense University, Madrid, Spain)

Education and former professional experience
-Bachelor´s degree in Chemistry with honors in 2000 (Complutense University, Madrid, Spain)
-PhD in Organic Chemistry under the guidance of Prof. Diego Armesto in 2005 (Complutense University, Madrid, Spain)
-Postdoctoral research associate at Complutense University under the supervision of Prof. María L. López-Rodríguez from 2005 to 2007
-Postdoctoral research associate at Imperial College London (United Kingdom) with a MEC scholarship under the supervision of Prof. Susan E. Gibson in 2008

Research field
Areas of interest: synthetic and medicinal chemistry, chemical biology
Research lines: neurodegenerative diseases (serotonin receptors), cancer (isoprenylcysteine carboxyl methyltransferase), antibacterial agents (bacterial cell division protein FtsZ), and development of chemical probes for the study of G protein-coupled receptors.

Fragment-Based Design of Inhibitors of The Antituberculotic Target 1-Deoxy-D-Xylulose-5-Phosphate Synthase Exploiting an Innovative Combination of NMR Techniques

Mrs Tiziana MASINI

UNIVERSITY OF GRONINGEN, Groningen, The Netherlands
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Mrs Tiziana MASINI

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Tiziana Masini studied chemistry at the University of Pisa, in Italy, where she received her Bachelor’s degree in Chemistry in 2007 and her Master’s degree in Organic Chemistry in 2009 with a thesis about the development of a new synthetic route to isoflavanones via a palladium-catalyzed direct arylation of 4-chromanones and structural analogues. After that, she followed a 2nd level postgraduate master course in “Natural Organic Substances” at the University “La Sapienza”, Rome. In October 2010 she started her PhD in the group of Dr. Anna K. H. Hirsch at the Rijksuniversiteit of Groningen, the Netherlands, and her research interest lies in the field of rational design and synthesis of pharmacologically interesting molecules involved in “neglected diseases”. In particular, she is exploring different lead-identification methodologies such as structure-based design, virtual screening and phage display to find potential inhibitors for the first enzyme of the non-mevalonate pathway, 1-deoxy-D-xylulose-5-phosphate synthase (DXS).

Design, Synthesis and Application Of Fluorinated Amino Acids as Labels to Study the Membrane Active Peptides by Solid State 19F NMR

Dr Pavel MYKHAILIUK

ENAMINE LTD, Kyiv, Ukraine
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Dr Pavel MYKHAILIUK

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Pavel Mykhailiuk was born in Kerch, Ukraine in 1984. In 2000 he won a bronze medal at 32nd International Chemistry Olympiads, IChO (Copenhagen, Denmark). In 2008 he received PhD at Technical University of Karlsruhe (KIT, Germany) after working with Prof. Anne Ulrich. Thereafter, he joined the Kyiv National Taras Shevchenko University (Ukraine), where he obtained PhD in Chemistry under the supervision of Prof. Igor Komarov. Since then Pavel holds a position Research Team Leader at the university with partial teaching. Independently, in 2009 he joined “Enamine LTD” company (Ukraine). In 2011 he became a head of custom synthesis department at Enamine; and since 2013 he holds a position of Chief Scientific Officer. Pavel´s research interests include fluorine-containing compounds, conformationally restricted molecules, 3D-shaped unnatural scaffolds and their application in medicinal chemistry. He is co-author of ca. 50 research manuscripts, 1 patent and 1 book chapter.

Rapid Kinase SAR Generation: an Integrated Approach to Synthesis, Screening and Molecular Design

Dr David PARRY

CYCLOFLUIDIC LTD, United Kingdom
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Dr David PARRY

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Dave has over 17 years’ experience in pharmaceutical discovery within the biotech and biopharmaceutical industry. Starting his career as a medicinal chemist he rapidly developed an enduring interest in small molecule discovery technologies having been responsible for diverse discovery functions including high throughput chemistry, analytical chemistry and the computational chemistry groups; prior to joining Cyclofluidic as the first employee Dave was Director, Technologies at UCB. The Cyclofluidic approach encompasses many of Dave’s research interest and he is now focussed on demonstrating the benefits that an integrated approach to small molecule discovery can provide to both pharma and biotech. Dave has a chemistry degree from Durham, UK; PhD in organic chemistry from Exeter and spent 2 years as a post doctoral fellow with Prof. Philip Magnus at UT, Austin, Texas.

Virtual Screening and Design of New Pharmaceutical Agents Using PASS Approach

Prof. Vladimir POROIKOV

INSTITUTE OF BIOMEDICAL CHEMISTRY, Moscow, Russia
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Prof. Vladimir POROIKOV

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Current title and position: Head of Department for Bioinformatics of the Orekhovich Institute of Biomedical Chemistry of Russian Academy of Medical Sciences, Professor of Medical-Biological Faculty at the N.I. Pirogov Russian National Research Medical University. Research fields: bioinformatics, chemoinformatics, (Q)SAR, molecular modelling and computer-aided drug design & discovery. Education and former professional experience: M.Sci. in Physics at Physical Faculty of the M.V. Lomonosov Moscow State University (1974); Ph.D. in Biophysics at Biological Faculty of the M.V. Lomonosov Moscow State University (1981); Dr.Sci. in Pharmacology at National Research Center for Biologically Active Compounds (1995).

Discovery of Highly Potent S1P1 Receptor Antagonists with in vivo Efficacy

Dr Jean QUANCARD

NOVARTIS, Basel, Switzerland
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Dr Jean QUANCARD

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Current Position: Project Team Leader at the Novartis Institute Biomedical Research Research Field: Medicinal chemistry Jean Quancard got in PhD in Chemistry at University Pierre et Marie Curie in Paris, France in 2004. He then moved to Stanford University in the US for a Postdoc in the group of Barry Trost. He then joined Novartis in 2006 as a Medicinal chemist in Basel where he worked in the field of autoimmune diseases and Oncology. Currently, he is part of an expertise platform focusing on proteases as drug targets.

Self-Immolative Spacers in Prodrug/Profluorophore Strategies: Determination of Kinetic Parameters for Release of Single or Multiple Substrates.

Dr Frédéric SCHMIDT

INSTITUT CURIE, Paris, France
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Dr Frédéric SCHMIDT

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He is involved in Medicinal Chemistry and Chemical Biology projects His research interests are mainly targeting strategies for antitumor agents, self-immolative spacers, bioconjugation (protein coupling techniques), and kinase inhibitors. He studied Chemistry at the Ecole Normale Supérieure, in Paris (1979-1983), and then entered CNRS as junior scientist. He obtained his PhD (1988) in the field of Supramolecular Chemistry under the supervision of Pr. Jean-Marie LEHN at the Collège de France. After a postdoc in the USA (Cornell University, Prof. John Mc MURRY), he moved in 1990 to ROUSSEL-UCLAF Laboratories (Romainville, France). In 1995, he joined the medicinal chemistry laboratory at the Institut Curie where he is still currently.

Discovery of Thienoimidazole-Based HCV NS5A Genotype 1a and 1b Inhibitors

Dr Graeme SMITH

VERTEX PHARMACEUTICALS, Cambridge, United States
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Dr Graeme SMITH

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Simon Giroux obtained his Ph.D in 2006 from the University of Montreal under the guidance of Prof. Stephen Hanessian. Following a 2-year NSERC postdoctoral fellowship at Harvard University (with Prof. E. J. Corey), he joined the Medicinal Chemistry Department at Vertex Pharmaceuticals (Cambridge, Massachusetts). Since 2009, he has been involved in research programs in different areas such as oncology, HCV and inflammation.

Synthetic Approach to Novel Melatonin Receptor Ligands

Mrs Maria VOLKOVA

MOSCOW STATE UNIVERSITY, CHEMISTRY DEPARTMENT, Moscow, Russia
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Mrs Maria VOLKOVA

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Current title and position: PhD Student in Medicinal Chemistry, Moscow State University, Russia. Research fields: Medicinal chemistry, Organic chemistry. Current research deals with Synthesis of novel melatonin receptor ligands and development of synthetic paths toward variable melatonin derivatives. Education: Since 2004 to 2009 – Student at the Chemistry department of Moscow State University, then PhD Student, Nikolay Zefirov’s Laboratory of Organic Syntheses, Chemistry Department, Moscow State University.