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Opening Lecture
Opening Lecture
The Art and Science of Total Synthesis and its Impact on Biology and Medicine: From the Fundamentals to the Translational (T01)
| Prof. K.C. NICOLAOU (RICE UNIVERSITY, Houston, United States) Read more
K. C. Nicolaou is currently the Harry C. Olga K. Wiess Professor of Chemistry at Rice University. He previously served concurrently as the founding chairman of the Chemistry Department at the Scripps Research Institute, a distinguished Professor of Chemistry at the University of California, San Diego (1989-2013), and the founding Director of the Chemical Synthesis Laboratory at ICES, A*STAR at Biopolis, Singapore. His research activities focus on the discovery and development of new synthetic strategies and technologies, and their applications to the total synthesis of natural and designed molecules of biological and medical importance. He is a co-author of the Classics in Total Synthesis series (I, II, III) and Molecules that Changed the World. Close window
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Invited Speakers
Flow Chemistry and Photochemistry as a Tool for Drug Discovery (T23)
| Dr Jesus ALCAZAR (JANSSEN RESEARCH & DEVELOPMENT, Toledo, Spain) Read more
Jesús Alcázar studied in Universidad de Castilla-La Mancha in Ciudad Real where he got his bachelor degree in 1990 and Ph. D. in 1996. As Ph. D. student he stayed for 6 months at the Royal Danish School of Pharmacy (Copenhagen, Denmark) under the direction of Prof. Michael Begtrup.
In 1995 he joined Janssen-Cilag at the research center in Toledo. Currently he is Senior Principal Scientist at Janssen Research and Development. In this position he is involved in the implementation of novel technologies in Drug Discovery in Toledo and in collaboration with other J&J sites worldwide. In this role he has led the successful implementation of 3 different technologies: microwave, H-CUBE and Flow chemistry, technologies that are currently a common tool at J&J worldwide. In addition, he has successfully applied these technologies to Medicinal Chemistry programs with 4 compounds selected as clinical candidates.
In the field of catalysis, he has made important contributions in the field of supported catalysis as well as the discovery of light induced cross coupling reactions.
He has been author of 5 book chapters and around 65 articles. He is inventor in around 35 patent applications.
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Awareness of PAINS (Pan Assay Interference Compounds) can Accelerate the Drug Discovery Process (T14)
| Prof. Jonathan BAELL (MONASH UNIVERSITY, Parkville, Australia) Read more
Jonathan Baell obtained his PhD in 1992 under Professors Peter Andrews and Paul Alewood at the Victorian College of Pharmacy (now MIPS) and went on to become a senior research scientist in CSIRO, Australia’s national scientific research organisation. Then, after a decade as head of medicinal chemistry at the Walter and Eliza Hall Institute of Medical Research (WEHI), he was appointed as a research professor at MIPS.
His interests are in the design of quality of HTS libraries, medicinal chemistry hit-to-lead and lead optimization, and computer-aided peptidomimetic design. Apart from his publications, he has over 40 granted pharmaceutical patents with compounds in various stages of development and clinical trial.
In 2005 he was awarded the 2004 RACI Biota Medal, a national award for excellence in medicinal chemistry for an early to mid-career researcher, followed by the Adrien Albert Medal for sustained medicinal chemistry excellence, in 2018. He sits on numerous scientific and editorial advisory boards, including Journal of Medicinal Chemistry, and is co-Senior Editor of Future Medicinal Chemistry.
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Artificial Intelligence in ADMET Modeling and Compound Profiling (T15)
| Dr Karl-Heinz BARINGHAUS (SANOFI, Frankfurt, Germany) Read more
Karl-Heinz Baringhaus obtained his Ph.D. in synthetic organic chemistry at the University of Muenster. After a postdoctoral fellowship at Stanford University he joined Hoechst AG where he was working in Medicinal Chemistry. In 2000 he became Head of Computational Chemistry at Aventis Pharma. From 2005 to 2010 he was Director of Drug Design at Sanofi-Aventis Pharma Deutschland GmbH. In 2010 he was promoted to Head of Structure, Design & Informatics consisting of Computational Biology & Bioinformatics, Computer-aided Drug Design, Scientific Computing & Data Management as well as Structural Biology. In 2012 Karl-Heinz was appointed R&D Site Director at Sanofi in Germany. Close window
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TLR7/8 Antagonists: from Screening to in vivo Potency (T26)
| Dr Claudia BETSCHART (NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland) Read more
Claudia Betschart received her PhD in natural sciences from the department of chemistry at the Swiss Federal Institute of Technology (ETH) in Zürich, Switzerland. After postdoctoral studies in Mexico City and at Colorado State University in Fort Collins, she started her carrier as a medicinal chemist end of 1991 with Ciba-Geigy (now Novartis) in Basel, Switzerland. Since then she contributed to drug discovery projects in various disease areas, including neuroscience, bone metabolism, and autoimmunity.
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RNA Therapeutics: New Chemical Modalities Becoming a Therapeutic Reality (T25)
| Dr Konrad BLEICHER (F.HOFFMANN-LA ROCHE LTD, Basel, Switzerland) Read more
Konrad Bleicher holds a Ph.D. in Organic Chemistry which he received from the Tübingen University in Germany. He started his professional career at Sandoz/Novartis (Switzerland & US) where he gained experience in the area of Combinatorial Chemistry before joining Roche as a scientist in the CNS chemistry department. Since then he has been holding various positions in the Small Molecule Medicinal Chemistry area (Hit ID, Lead ID & Lead Optimization). In 2009 Dr. Bleicher was nominated “Peptide Area Head”, overseeing the peptide chemistry activities in Pharma Early Research & Development. Since 2016 he is responsible for the RNA Therapeutics Chemistry strategy and platform development in Roche Basel. He is the author of over 60 patents and publications and an invited speaker for various international conferences. Close window
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Sustainable by Design Anti-Trypanosomatid Small Molecules: an Aspirational Goal for Medicinal Chemistry (T16) - ChemMedChem Lecture
| Prof. Maria Laura BOLOGNESI (UNIVERSITY OF BOLOGNA, Bologna, Italy) Read more
Maria Laura Bolognesi is Professor of Medicinal Chemistry, Director of the Chemistry and Pharmaceutical Technologies degree program and Rector Delegate for Latin American International Relations at the University of Bologna. She obtained her PhD under the mentorship of Professor Carlo Melchiorre in 1996 and carried out postdoctoral work at the University of Minnesota with Professor Philip S. Portoghese. Her research explores the development of small molecules in the neurodegenerative and neglected tropical disease therapeutic areas. Maria Laura was awarded the positions of Distinguished Visiting Professor at the Complutense University of Madrid in 2009, Pesquisador Visitante Especial at the University of Brasilia in 2014 and Professeur Invité at Université Caen Normandie in 2018. She is an Associate Editor of Journal of Medicinal Chemistry and serves in the Advisory Board of the European Federation of Medicinal Chemistry Close window
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Catalytic Chirality Generation: New Strategies for Organic Synthesis (T06)
| Prof. John BOWER (UNIVERSITY OF BRISTOL, Bristol, United Kingdom) Read more
John F. Bower obtained his MSci degree in 2003 from the University of Bristol, where he remained to study for his PhD degree (2007) under the guidance of Professor Timothy Gallagher. He then undertook postdoctoral appointments with Professor Michael Krische at the University of Texas at Austin (2007-2008) and Professor Timothy Donohoe at the University of Oxford (2008-2010). In 2010, he was awarded a Royal Society University Research Fellowship and commenced his independent career at the University of Bristol. The group’s research interests lie broadly within the area of synthetic chemistry, with a focus on N-heterocyclic methodologies and metal-catalysed processes. Bower’s research has been recognized by a number of awards, including the 2013 Royal Society of Chemistry Harrison-Meldola Memorial Prize, the 2015 Royal Society of Chemistry Hickinbottom Award and a 2016 Philip Leverhulme Prize. Close window
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Nature’s Medicine Chest: Opportunities for Synthesis and Drug Discovery (T02)
| Prof. Margaret Anne BRIMBLE (THE UNIVERSITY OF AUCKLAND, Auckland, New Zealand) Read more
Margaret Brimble is the Director of Medicinal Chemistry and a Distinguished Professor at the University of Auckland, New Zealand where her research program focuses on the synthesis of bioactive natural products, antimicrobial peptides, cancer vaccines, glycopeptides, self-assembling peptides and peptidomimetics. She has published >460 papers, 60 reviews and is an inventor on >30 patents. In 2018 she was elected a Fellow of the Royal Society London and was awarded the Royal Society of Chemistry George and Christine Sosnovsky Award in Cancer Therapy. She won the 2016 Marsden Medal, the 2012 RSNZ Rutherford (NZ’s top science prize), MacDiarmid and Hector Medals, the 2011 Royal Australian Chemical Institute Adrien Albert Award, the 2010 RSC Natural Products Award, the 2007 L’Oreal-UNESCO Women in Science laureate in Materials Science for Asia-Pacific, a 2015 IUPAC Distinguished Women in Chemistry/Chemical Engineering Award and conferred the Queen’s Honour CNZM. She is Past-President of IUPAC Organic and Biomolecular Division III, an Associate Editor for Organic and Biomolecular Chemistry, Past-President of the International Society of Heterocyclic Chemistry and Past-Chair of the Rutherford Foundation RSNZ. She discovered the first drug named “trofinetide” to treat Rett Syndrome and Fragile X syndrome that is in phase III clinical trials with Neuren Pharmaceuticals. Trofinetide is New Zealand’s first successful drug and one of only a few to be discovered in an academic laboratory. Margaret also co-Founded the spin-out company SapVax with US$6 million funding from BioMotiv USA to take self-adjuvanting cancer vaccines based on a novel chemistry platform, to clinical trial (see: https://sapvaxllc.com). Close window
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Allosteric Activation of a Master Metabolic Regulator AMPK: Drug Discovery Opportunities and Challenges (T27)
| Dr Kimberly CAMERON (PFIZER, Cambridge, United States) Read more
Kimberly Cameron is a Research Fellow in Medicine Design at Pfizer. Kimberly obtained a B.A. at Rutgers University and a Ph.D. in organic chemistry at the University of Colorado in Boulder, where she discovered Lewis acid-promoted annulation reactions working with Prof. Gary A. Molander. Kimberly is a globally recognized drug discovery expert and has led chemistry and interdisciplinary teams targeting diverse biology space including AMPK, ghrelin, prostaglandin receptors and nuclear hormone receptors. Kimberly’s research interests include medicinal chemistry, organic chemistry, kinases, orphan GPCRs, structure-based drug design, and tissue-targeted therapies. Close window
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Design and Synthesis of Chemical Probes for Bromodomains (T10)
| Prof. Stuart CONWAY (UNIVERSITY OF OXFORD, Los Angeles, United States) Read more
Stuart Conway is a Professor of Organic Chemistry at the University of Oxford, and the E. P. Abraham Cephalosporin Fellow in Organic Chemistry at St Hugh's College, Oxford. He studied Chemistry with Medicinal Chemistry at the University of Warwick before undertaking PhD studies with Professor David Jane and Professor Jeff Watkins FRS at the University of Bristol. Stuart completed post-doctoral studies with Professor Andrew Holmes FRS at the University of Cambridge. In 2003, he was appointed as a Lecturer in Bioorganic Chemistry at the University of St Andrews, in 2008 was appointed as an Associate Professor at Oxford, and in October 2014 he was promoted to Full Professor. Between March and August 2013 Stuart was a Visiting Associate at the California Institute of Technology. Since 2016 he has been an Associate Editor for the Journal of Medicinal Chemistry and he is the President-elect of the RSC Organic Division. His research focuses on the development of chemical tools to study biological systems. Close window
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Start Selective and Rigidify: The Discovery Path Towards the Next Generation of EGFR Tyrosine Kinase Inhibitors (T24)
| Dr Harald ENGELHARDT (BOEHRINGER-INGELHEIM, Vienna, Austria) Read more
Research field: Oncology
Professional experience and education:
Since 01/2003 Project leader for international and interdisciplinary research projects
Since 01/2001 Principal Scientist Medicinal Chemistry at Boehringer Ingelheim RCV GmbH & Co KG
05/1998 – 12/2000 Lab Scientist at Boehringer Ingelheim Pharma KG
08/2008 – 12/2013 PhD thesis under the supervision of Prof. Dr. R. Leurs and Prof. Dr. E. E. J. Haaksma with the title "Design and preparation of new ligands interacting with the Histamine H4 receptor" at the VU University Amsterdam and at Boehringer Ingelheim RCV GmbH & Co.
10/1997 – 02/1998 Diploma thesis under the supervision of Prof. Dr. T. Herold and Dr. L. Kisielowski
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Artificial Intelligence in de Novo Molecular Design (T17)
| Dr Ola ENGKVIST (ASTRAZENECA, Mölndal, Sweden) Read more
After he completed his PhD in Computational Chemistry at the University of Lund and postdoctoral research at the University of Cambridge and the Czech Academy of Sciences, he joined AstraZeneca in 2004. He currently leads the Discovery Sciences Computational Chemistry team within the IMED Biotech Unit, providing computational solutions for drug discovery.
He is passionate about pushing the boundaries of using artificial intelligence and machine learning in drug discovery. A key focus for him has been on building both the team within IMED and collaborating with external experts to advance innovation in drug design and synthesis.
Through a pioneering collaboration with the University of Muenster, his team demonstrated the first application of recurrent Neural Networks to molecular design which has been published in two recent, highly-cited articles. This methodology allows them to design novel drug molecules using machine learning to navigate the breadth of chemical space and to exploit their vast knowledge base. Close window
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Design and Implementation of de Novo Biosynthetic Cascades (T20)
| Prof. Sabine FLITSCH (UNIVERSITY OF MANCHESTER, Manchester, United Kingdom) Read more
Sabine has a long-standing interest in the application of biocatalysis to organic synthesis. More recently, she has developed multistep cascade reactions mediated by enzymes, both in cell free and whole cell systems for the stereoselective synthesis of carbohydrates and amines.
Sabine obtained a Diploma in Chemistry from the University of Muenster, Germany and a DPhil degree from Oxford University under the supervision of Sir J E Baldwin. She spent three years of postdoctoral studies with Professor H G Khorana at MIT before returning to the UK to pursue her academic career at the Universities of Exeter, Oxford, Edinburgh and now Manchester, where she has held a Chair since 2004.
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Catalysis for Total Synthesis (T21)
| Prof. Alois FÜRSTNER (MAX PLANCK INSTITUT FUR KOHLENFORSCHUNG, Muelheim an der Ruhr, Germany) Read more
Alois Fürstner studied chemistry in Austria where he obtained his doctoral degree in 1987 from the Technical University of Graz (Prof. H. Weidmann). After a postdoctoral stint with the late Prof. Oppolzer in Geneva, Switzerland, and a Habilitation in Graz, he joined the Max-Planck-Institut für Kohlenforschung, Mülheim, Germany, in 1993 as a group leader. In 1998, he was promoted to the rank of Director of this Institute and served as its Managing Director in 2009-2011 and 2016-2017.
His scientific interests relate to organometallic chemistry and homogeneous catalysis, including applications thereof to target oriented synthesis. Long term projects are focused on alkene- and alkyne metathesis, pi-acid catalysis based on platinum and gold, iron catalyzed cross coupling, and carbene chemistry in general. These methods opened concise and flexible entries into numerous bioactive natural products (alkaloids, macrolides, prostaglandins, glycolipids).
For a short personal account, see: Angew. Chem. Int. Ed. 2014, 53, 8587
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Amides and Chemical Education as Vehicles for Innovation (T18)
| Prof. Neil GARG (UNIVERSITY OF CALIFORNIA, Los Angeles, United States) Read more
Neil Garg received a B.S. in Chemistry from New York University where he did undergraduate research with Professor Marc Walters. He obtained his Ph.D. in 2005 from Caltech studying under the direction of Professor Brian Stoltz. Garg then joined Professor Larry Overman’s laboratory at the University of California, Irvine as an NIH Postdoctoral Scholar. Garg joined the faculty at UCLA in 2007. He was promoted to Associate Professor in 2012, and then to Full Professor in 2013. He has served as Vice Chair for the Department of Chemistry and Biochemistry (2012-2016) and currently serves as Faculty-in-Residence in the UCLA undergraduate community. In 2018, Garg was appointed as the inaugural holder of the Kenneth N. Trueblood Endowed Chair in Chemistry and Biochemistry.
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A Chemical Approach to Map Protein Interactions at the Cell Surface (T12)
| Dr Erik HETT (MERCK EXPLORATORY SCIENCE CENTER, Boston, United States) Read more
Dr Erik Hett received his Ph.D. from Harvard University in the lab of Dr Eric Rubin, studying protein-protein interactions important for regulating cell division in mycobacteria. His postdoctoral research was conducted in the lab of Dr Deborah Hung at Harvard, Broad Institute and Massachusetts General Hospital, where he conducted phenotypic high-throughput screens and utilized chemoproteomics for target ID. He previously was a chemical biologist in the MedChem Department at Pfizer and led a chemical biology team in the mechanisms and pathways group at Biogen. He is currently the Head of Experimental and Chemical Biology at Merck’s Exploratory Sciences Center in Cambridge, MA. Close window
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A Medicinal Chemist's Perspective on Solute Carriers: Avoiding or Targeting them (T11)
| Dr Kim HUARD (GENENTECH, San Francisco, United States) Read more
Dr Kim Huard recently joined Genentech in South San Francisco where she leads chemistry teams on drug discovery programs. In 2008, she graduated from the Université de Montréal with a Ph.D. in organic chemistry where she developed a rhodium-catalyzed carbon-hydrogen bond nitrene insertion methodology. Following her graduate studies, Kim contributed to the total synthesis of the structurally complex natural product daphnipaxinin as a FQRNT postdoctoral fellow at the University of California, Irvine. Kim joined Pfizer in 2010 as a medicinal chemist in the cardiovascular and metabolic disease research unit. Since 2012, she has been leading teams on various drug discovery programs which led to the discovery of three clinical candidates. Her work involves modulation of different types of biological targets with small molecules as well as targeting specific compound disposition such as liver selective or brain penetrant agents. Close window
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Practical Heteroatom- and Group-Transfer Reactions (T09)
| Dr Laszlo KURTI (RICE UNIVERSITY, Houston, United States) Read more
László Kürti was born and raised in Hungary. He received his Diploma from Lajos Kossuth University (now University of Debrecen) where he conducted research in the laboratory of Professor Sándor Antus focusing on the total synthesis of benzofuranoid neolignans. Subsequently he received his Master of Science degree at the University of Missouri-Columbia, working with Professor Michael Harmata on inter- and intramolecular [4+3]-cycloadditions of halogen-substituted oxoallylic cations, and his Ph.D. degree (2006) in synthetic organic chemistry under the supervision of Professor Amos B. Smith III at the University of Pennsylvania where he developed a new method for the construction of highly substituted and strained indoles that was applied in the synthetic studies toward the construction of the complex indole diterpenoid natural products, nodulisporic acids A and B.
While still in graduate school he authored the now popular textbook/reference book "Strategic Applications of Named Reactions in Organic Synthesis" with Barbara Czakó that is now used in dozens of academic institutions and research laboratories worldwide.
In 2006 László joined the group of Professor E.J. Corey at Harvard University as a Damon Runyon Cancer Fellow where he was working on the development of potent antiangiogenic agents inspired by the structure of Cortistatin A. In 2007 he co-authored the book "Molecules and Medicine" with Professor E.J. Corey and Dr. Barbara Czakó. In February 2008, the Professional and Scholarly Division of the American Association of Publishers designated Molecules and Medicine “Best of Physical Sciences and Mathematics”. In the Fall of 2010, László and Prof. Corey self-published “Enantioselective Chemical Synthesis: Methods, Logic and Practice” that was warmly received by the community. Now this book is sold by Elsevier/Academic Press.
László began his independent career as an Assistant Professor in the Department of Biochemistry at UT Southwestern Medical Center, Dallas, Texas, but on June 1, 2015 he joined the faculty at Rice University (Houston, Texas); now he is a tenured Associate Professor in the Department of Chemistry. László’s laboratory is located in the BioScience Research Collaborative (BRC) building that has state of the facilities and offers many opportunities for collaborations.
The Kürti group focuses on the development of powerful new methods for the expedient enantioselective assembly of highly functionalized biaryls, heterocycles and carbocycles. Thus the group has been exploring several fundamentally new strategies for the transition-metal-free direct: (i) arylation of arenes; (ii); alpha-arylation of ketones, esters and amides; (iii) O-arylation of oximes; (iv) primary amination of arylboronic acids and (v) inter- and intramolecular C(sp2)-H amination of arenes. In-depth experimental and computational studies have already identified the critical factors required for efficient alkyl-aryl, aryl-aryl, O-aryl, N-alkyl and N-aryl bond-formation and led to several innovative and environmentally benign methods for the rapid preparation of structurally diverse arylated carbonyl compounds, functionalized biaryls as well as O- and N-heterocycles. Recently, László has been the recipient of an NSF CAREER Award, Fellowship by the Japan Society for the Promotion of Science (JSPS), the 2014 Amgen Young Investigators’ Award as well as the 2015 Biotage Young Principal Investigator Award.
Besides being engaged in research, teaching and writing, in his free time László travels all over the world with his wife and son and enjoys learning about other cultures and people. So far he has visited 37 countries on five continents and 38 states in the US.
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Discovery of AZD5718, a Novel 5-lipoxygenase Activating Protein (FLAP) Inhibitor (T19)
| Dr Malin LEMURELL (ASTRAZENECA, Gothenburg, Sweden) Read more
Malin Lemurell achieved her PhD at the Gothenburg University in 1999 in organic chemistry, specialized on bio-catalyzed asymmetric transformations. After post-doctoral studies on metal catalyzed asymmetric oxidation at The Scripps Research Institute in California with Prof. Barry Sharpless, she continued her career in medicinal chemistry as scientist and later leader at AstraZeneca, Gothenburg, Sweden. Malin is the inventor of 13 patents, incl patents behind the launched medicine Elobixibat and currently two other compounds in Phase II clinical development.
Research Field: Medicinal Chemistry with long experience in the Cardiovascular, Renal and Metabolism disease areas and with special interest in drug design, innovations in the interface of chemistry and biology including new chemical modalities and targeted drug delivery, as well as development of drug hunters of the future
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Photoinduced Assembly of C–N Bonds (T08)
| Prof. Daniele LEONORI (UNIVERSITY OF MANCHESTER, Aachen, Germany) Read more
Daniele obtained his PhD at the University of Sheffield under the supervision of Professor Iain Coldham (2010). After postdoctoral studies with Professor Magnus Rueping (RWTH Aachen University) and with Professor Peter H. Seeberger (Max Planck Institute) he joined the group of Professor Varinder K. Aggarwal FRS as Research Officer (University of Bristol). In 2014 he commenced his independent career as Lecturer in Organic Chemistry at the University of Manchester and was promoted to Reader in 2018. The group’s main research interests are in the area of catalysis and synthetic chemistry, with a focus on the assembly of N-containing molecule. Daniele was awarded an EPSRC Early Career Fellowship in 2016, the ERC Starting Grant in 2017 and the RSC Harrison-Meldola Memorial Prize in 2018. Close window
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Discovery of First in Class, Orally Bioavailable p300/CBP HAT Domain Inhibitors (T04)
| Dr Michael MICHAELIDES (ABBVIE, North Chicago, United States) Read more
Michael earned his B.Sc. degree in chemistry from Stony Brook University and his doctorate in organic chemistry from the Massachusetts Institute of Technology. He joined Abbott immediately after completing his graduate studies.
During his 30-year tenure at Abbott and now Abbvie, Michael has carried out research in the areas of Neuroscience, Immunoscience and Oncology. He has contributed to the invention and advancement of several clinical candidates, including adrogolide for the treatment of Parkinson’s disease and linifanib for hepatocellular carcinoma. He has over 40 issued patents and over 50 published articles to his name.
Michael is currently Senior Research Fellow, Senior Director of Oncology Chemistry and a member of the Global Abbvie Medicinal Chemistry Leadership Team.
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Drug Discovery in Academia (T03)
| Prof. Oliver PLETTENBURG (LEIBNIZ UNIVERSITY HANNOVER, Hannover, Germany) Read more
Oliver Plettenburg, PhD, is full professor for ‘Medicinal Chemistry’ at Leibniz Universität Hannover and director of the Institute of Medicinal Chemistry of the Helmholtz Center Munich. Before rejoining academia he spent more than fourteen years in a major pharmaceutical venture, last he held positions as “Head of Chemical Biology” and “Head of Biosensors and Chemical Probes”. His research focuses on hit and lead optimization of promising compounds for treatment of devastating diseases, development of innovative targeted and smart drug delivery methods and synthesis of novel imaging agents for in-vivo monitoring of pathogenesis.
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From Fragments to Antibody Drug Conjugates in Emerging Oncology Targeted Therapies (T13)
| Dr Laurent SCHIO (SANOFI, Vitry sur Seine, France) Read more
Laurent Schio is currently head of Integrated Drug Discovery of Sanofi in France. He supervises groups of medicinal chemistry, drug design, structural biology, screening and data management. He is organic chemist by training. He obtained his PhD degree from the University of Rennes (Britany-France) in 1990 in Dr René Gree’s laboratory (iron tricarbonyle complexes). He performed then a postdoctoral stage in Pr. Joshua Rokach’s laboratory (synthesis of isoprostaglandins) in the Florida Institute of Technology (Melbourne). He joined then Sanofi (Roussel-Uclaf) in 1991. His main therapeutic domains of expertise are the anti-infective and oncology areas and contributed to the discovery of several clinical candidates (Aminocandin, cMET, PI3Kb, SERD...). He is author of more than 25 publications, co-inventors in 20 patents and has realized more than 20 oral presentations worldwide. He is currently member of the Sanofi French Hub and the Oncology Discovery Boards. Close window
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Nucleophilic Boron for the Synthesis of Functionalized Small Rings (T07)
| Prof. Mariola TORTOSA (AUTONOMOUS UNIVERSITY OF MADRID, Madrid, Spain) Read more
Mariola Tortosa obtained her PhD at the Organic Chemistry Institute (CSIC, Madrid, Spain) under the supervision of Professor Fernández de la Pradilla (2005). In 2005, she moved to The Scripps Research Institute in Florida (USA) to work as a Postdoctoral Fellow with Prof. William R. Roush. In 2008 she returned to the Organic Chemistry Institute (Madrid, Spain) as a Research Assistant. In 2011 she started her independent career at the Universidad Autónoma de Madrid (UAM) as an Assistant Professor (Ramón y Cajal Fellow). More recently, she received an ERC-Starting Grant awarded by the European Research Council to work on the project “Design and Applications of Unconventional Borylation Reactions”. In 2017, she was promoted to Associate Professor at UAM. Biologically active compounds (natural products and drugs) are a continuous inspiration for her research which includes asymmetric catalysis, boron chemistry and the development of metal-catalyzed transformations. Close window
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Development and Application in Flow of Sustainable Synthetic Methodologies that Use Singlet Oxygen as Green Oxidant and Cascade Reaction Facilitator (T22)
| Prof. Georgios VASSILIKOGIANNAKIS (UNIVERSITY OF CRETE, Heraklion, Greece) Read more
Georgios Vassilikogiannakis is Full Professor of Organic Chemistry at the Department of Chemistry of the University of Crete. He obtained his Ph.D. (1998) in Physical Organic Chemistry with Prof. M. Orfanopoulos from the University of Crete (Greece). From 1999-2002, he was a postdoctoral fellow at the Scripps Research Institute (California, U.S.A.) in the group of Prof. K. C. Nicolaou.
In 2002 he started his academic career at the University of Crete initially as an Assistant Professor. In 2008, he was promoted to Associate Professor, and, in 2013, to Full Professor.
He is the recipient of an ERC Consolidating grant and an ERC Proof of Concept grant.
His research interests are in the field of Sustainable Synthetic Organic Chemistry with a particular focus on: a) The development and application of new green synthetic methodologies that use Singlet Oxygen as a green oxidant and cascade reaction facilitator and b) the continuous flow photochemisty.
You can find more information in the website: http://www.chemistry.uoc.gr/vassilikogiannakis/
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Novel Bacterial Topoisomerase Inhibitors (NBTI) with Potent Gram-Negative Activity (T05)
| Dr Cornelia ZUMBRUNN (IDORSIA PHARMACEUTICALS, Allschwil, Switzerland) Read more
Cornelia Zumbrunn holds a position as Principal Scientist (medicinal chemist and project leader) in the field of antibacterial research and cardiovascular diseases. Since 2004 she worked in the research department of Actelion Pharmaceuticals Ltd, now Idorsia Pharmaceuticals Ltd. (Allschwil, Switzerland). Previous positions include Morphochem AG and Hoffmann-LaRoche, after a postdoc at Cambridge University (UK).
Cornelia obtained her PhD from Hoffmann-LaRoche and the University of Zürich after having completed studies in organic chemistry in Fribourg (CH) and Neuchâtel (CH).
Her research focused on the discovery of antibiotics with novel modes of action and other projects in the areas of central nervous systems and cardiovascular research.
She is a board member and the secretary of the Division of Medicinal Chemistry and Chemical Biology of the Swiss Chemical Society (DMCCB).
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Oral Communications
Rapid Exploration of Synthetically Tractable Chemical Space and Lead Optimization Using a Combination of Reaction-Based Enumeration, Active Learning, and Free Energy Calculations (OC02)
| Dr Tatjana BRAUN (SCHRÖDINGER, Mannheim, Germany) Read more
Tatjana Braun has studied Bioinformatics at the Technical University and the Ludwig-Maximilian University of Munich. She then obtained her doctorate from the University of Düsseldorf for research mainly focusing on structure modelling using cryo-EM data. In 2017, she joined Schrödinger to work as an Applications Scientist. Close window
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Developing a ‘Reverse-Biomimetic’ Synthesis of Arogenate and its Analogues (OC09)
| Ms Louise EAGLING (UNIVERSITY OF BRISTOL, Bristol, United Kingdom) Read more
Louise Eagling obtained her MChem degree in 2015 from the University of East Anglia. As part of her degree, she undertook an industrial placement working for Novartis as a medicinal chemist. Her final year project was carried out under the supervision of Dr. Paz Muńoz-Herranz, in collaboration with Novartis, exploring the platinum catalysed inter- and intramolecular addition of nucleophiles to allenes to obtain multi-heteroaromatic structures with potential biological activity. She is currently working towards her PhD at the University of Bristol under the supervision of Prof. Jonathan Clayden as part of the Chemical Synthesis CDT with CASE sponsorship from Syngenta. Her PhD has focussed on the total synthesis of Arogenate and derivatives with potential agrochemical or medicinal applications. Close window
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Macrocyclic Modalities for Modulation of Protein-Protein Interactions (OC06)
| Dr Stéphanie GUERET (ASTRAZENECA MPI SATELLITE UNIT, Mölndal, Sweden) Read more
After studying organic chemistry at the University Claude Bernard Lyon 1, France, Stéphanie Guéret completed her PhD in 2011 from the University of Auckland, New Zealand where she achieved the total synthesis of the spiroimine unit of the Spirolide family of natural products. She then joined the Novartis Institute for Biomedical Research (NIBR) in Basel, Switzerland as a presidential postdoctoral fellow and developed a new class of cyclic peptidomimetics.
In 2015 she took a senior research scientist position at AstraZeneca to join the AstraZeneca-Max Planck Institute Satellite Unit, embedded in the group of Prof. Waldmann in Dortmund, Germany. Together with a small team of students and scientists, she has led major projects of the satellite unit focusing on the synthesis development of mixed macrocycles to modulate protein-protein interactions and the use of “new modalities” such as stabilized peptides to address challenging targets.
Her current research interest is synthetic and medicinal chemistry with broadening towards chemical biology to solve key questions on how to move forward novel chemical modalities towards drug-like compounds.
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EFMC Prize for a Young Medicinal Chemist in Academia
From the Elucidation of the Mechanism of Vitamin E to the Design of Innovative Drugs that Limit Inflammation and Enhance Resolution (OC10)
| Dr Andreas KOEBERLE (UNIVERSITY OF JENA, Jena, Germany) Read more
Andreas Koeberle is research group leader and lecturer at the University of Jena (Germany). He graduated in biochemistry and received a Ph.D. in Medicinal Chemistry/Analytics at the University of Tuebingen (Germany) in 2009. After postdoctoral studies at the University of Tokyo (Japan), he joined the Chair of Medicinal/Pharmaceutical Chemistry at the University of Jena (Prof. Oliver Werz), where he established the institutional lipidomics facility. In 2018, he became visiting professor at the University of Vienna (Austria). Offers for full professorships followed in 2017 from the Paracelsus Medical University (Salzburg, Austria) and 2019 from the University of Innsbruck (Austria). His research focuses on the characterization of lipid signaling pathways at the interface of inflammation, cancer and homeostasis and on the identification of drug targets and leads with focus on natural products. Detailed information: https://www.pharmazie.uni-jena.de/Abteilungen.html Close window
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Stabilizing Inactive Conformations of MALT1 AS an Effective Strategy to Inhibit its Protease Activity (OC05)
| Dr Jean-Baptiste LANGLOIS (NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland) Read more
Jean-Baptiste Langlois obtained is PhD in organic chemistry from the University of Geneva (Switzerland), where he worked on asymmetric catalysis in the group of Prof. Alexakis. In 2012, he moved to the Massachusetts Institute of Technology (Cambridge, USA) to perform his post-doctoral studies with Prof. Buchwald. Jean-Baptiste came back to Switzerland in 2013 to start his career as medicinal chemist. First, in a startup company named PIQUR Therapeutics focusing on the discovery of new PI3K inhibitors and eventually at the Novartis Institutes for Biomedical Research in Basel. Over the past years, Jean-Baptiste acquired a quite diverse experience, working successively in the fields of autoimmune disorders, oncology and more recently on musculoskeletal diseases. Close window
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EFMC Prize Winner EFMC-YMCS 2018
Development of Release-And-Report Kinase Inhibitors as Molecular Tools for Investigating Neurodegenerative Disorders (OC04)
| Dr Cassandra LEE FLEMING (UNIVERSITY OF GOTHENBURG, Gothenburg, Sweden) Read more
Cassandra Fleming obtained her PhD in organic chemistry in 2015 from Deakin University, Australia. Following her doctorate, she joined the group of Prof Joakim Andréasson as a postdoctoral researcher at Chalmers University of Technology, in which her work focused on the development of fluorescent bioactives as molecular tools to probe real-time intracellular events. Cassandra currently works as a Marie Curie postdoctoral fellow at the University of Gothenburg in the group of Prof Morten Grřlti. Her research interests include the development of light responsive molecular tools for the study of disease progression in a cellular setting. Close window
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A Radical Approach for the Late-Stage Functionalization of Phosphinic Peptides (OC03)
| Mr Angelos LELIS (UNIVERSITY OF ATHENS, Athens, Greece) |
Practical and Asymmetric Gilman-Speeter Synthesis of B-Lactams (OC01)
| Prof. Plato MAGRIOTIS (UNIVERSITY OF PATRAS, Patras, Greece) Read more
Since 2006, Plato A. Magriotis, Ph.D., is an Associate Professor of Medicinal Chemistry in the Department of Pharmacy at the University of Patras in Greece and a Research Affiliate with the Department of Chemistry at New York University. Magriotis received his Ph.D. in Chemical Biology with Professor Francis Johnson at Stony Brook University in 1983 and did Postdoctoral work at Harvard University with Nobel Laureate Professor E. J. Corey. His career started at West Virginia University and continued at Merck & Co. as well as New York University in the U.S., prior to his return to Greece. Magriotis’ research program focuses on the development of new methodology for the synthesis of relevant pharmacophores applied in drug discovery. Close window
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Discovery of GSK701, a Novel Orally Effective Preclinical Drug Candidate for the Treatment of Malaria (OC08)
| Dr Jose Ignacio MARTIN (GSK, Tres Cantos, Spain) Read more
Born in Salamanca, he completed his studies at the University of Salamanca and then joined Dr S. Arseniyadis group at the Institut de Chimie des Substances Naturelles (ICSN-CNRS, France) for a first 3-year postdoctoral stage where he was involved in the total synthesis of taxoids and Lead tetraacetate mediated one-pot multistage transformations on unsaturated 1,2-diols. In 2000 he moved to USA and joined Prof. A. S. Kende group at the University of Rochester (NY) to deal with the first total synthesis of the alkaloids Stemonamide and Isostemonamide. In January 2002 Jose started working at Merck & Co as Senior Research Chemist in its Istituto di Ricerca di Biologia Moleculare at Pomezia (Italy) where he spent almost eight years working in hepatitis C and cancer. In November 2008 he returned to Spain to work at the Spanish National Cancer Centre (CNIO) for 3 years. Since 2012 he works at GSK in the Diseases for Developing World unit in the Malaria unit. Close window
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Removable Directing Groups for Late-Stage Functionalisation (OC12)
| Dr Miriam O'DUILL (NATIONAL UNIVERSITY OF IRELAND, Galway, Ireland) Read more
Miriam O’Duill obtained her MChem from the University of Oxford (Merton college) in 2011. In 2015, she completed her PhD at the same university under the supervision of Véronique Gouverneur, developing late-stage fluorination and perfluoroalkylation methodology with a view towards the radiolabelling of new PET tracers. After a two-year stint as a DAAD Postdoctoral Fellow with Keary M. Engle at the Scripps Research Institute in La Jolla, California, investigating transition-metal catalysed alkene functionalisation, Miriam joined the School of Chemistry at the National University of Ireland, Galway as a lecturer in January 2018. Close window
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Antimicrobial Activity of Curcumin Analog PGV-6, HGV-6 and GVT-6 (OC07)
| Prof. Leni RITMALENI (GADJAH MADA UNIVERSITY, Yogyakarta, Indonesia) Read more
Dr Ritmaleni received her PhD from the School of Chemistry, University of Bristol, United Kingdom in 2004, under supervision of Prof. V. K. Aggarwal. She was as a visiting scholar at Department of Chemistry, Graduate School of Science, Tohoku University, Japan in 2013 and visiting scientist at School of Pharmacy, University of Groningen, The Netherland in 2014. Now, she is appointed as a Director of Curcumin Research Center, Faculty of Pharmacy, Gadjah Mada University apart as Associate Professor at Faculty of Pharmacy, Gadjah mada University. She is a recipient of Elsevier Foundation Award 2014 in Chemistry, Study UK Alumni 2017 and ASEAN Science Leadership Program Fellow. She is a reviewer of Journal of Molecular Structure, Elsevier and reviewer of Chemistry Select, Wiley-VCH.
Her research interest is focused on the synthesis of active molecule as drug candidate especially curcumin analogs. She has collaboration with Prof. Tasuki Kaneko from TB Alliance, USA where she got funding for her research on antituberculosis activity of curcumin analog compounds. She also has collaboration with Prof. Herman Spaink from Leiden University, The Netherlands for in vitro/in vivo assay of antituberculosis activity of curcumin analogs by using Zebra Fish as a model.
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EFMC Prize for a Young Medicinal Chemist in Industry
Cipargamin-Biocatalysis in the Discovery and Development of an Antimalarial Drug (OC11)
| Dr Radka SNAJDROVA (NOVARTIS PHARMA AG, Basel, Switzerland) Read more
Radka obtained her PhD from Vienna University of Technology in 2007 where she worked on the asymmetric synthesis of lactones using a combination of chemical and biocatalytic approaches. She received an Erwin-Schroedinger Fellowship and spent 1 year of postdoctoral study at York University in the UK, exploring the development of novel biocatalysts for organosilane chemistry. In 2009, Radka moved to University of Greifswald, Germany as a senior postdoctoral fellow to develop a high-throughput screening approach for in vivo selection and cell sorting, with the primary goal of identifying novel enantioselective enzymes.
In 2011, she transitioned to industry with a one year role at a lab focused on supporting chemists at GSK to take advantage of biocatalytic technologies (Novacta), prior to directly joining Chemical Process Development at GSK, UK as Project leader responsible for the development and implementation of new biocatalytic technology in both pre- and post-commercialisation routes. Since Dec 2016, Radka is leading the Bioreactions group in Global Discovery Chemistry at Novartis Institute for Biomedical Research in Basel.
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