EFMC-ASMC'19

EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry

 Athens, Greece    September 1-5, 2019

Programme


09:00

Excursions - Tour 1

14:00

Excursions - Tour 2

15:30

Registration

17:30

Opening

Prof. Varinder K. AGGARWAL
UNIVERSITY OF BRISTOL, Bristol, United Kingdom
Dr Spiros LIRAS
BIOGEN, Cambridge, United States


Dr Yves P. AUBERSON
NOVARTIS & EFMC, Basel, Switzerland
Dr Gene VAISBERG
CHEMBRIDGE CORPORATION, San Diego, United States
Prof. Emmanuel MIKROS
UNIVERSITY OF ATHENS, Athens, Greece

18:00

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

19:00

Welcome Reception

20:00

End of the Day

08:00

Registration

Session Chair

Prof. Varinder K. AGGARWAL
UNIVERSITY OF BRISTOL, Bristol, United Kingdom

08:30

Nature’s Medicine Chest: Opportunities for Synthesis and Drug Discovery (T02)

Prof. Margaret Anne BRIMBLE
THE UNIVERSITY OF AUCKLAND, Auckland, New Zealand

09:15

Drug Discovery in Academia (T03)

Prof. Oliver PLETTENBURG
LEIBNIZ UNIVERSITY HANNOVER, Hannover, Germany

10:00

Practical and Asymmetric Gilman-Speeter Synthesis of B-Lactams (OC01)

Prof. Plato MAGRIOTIS
UNIVERSITY OF PATRAS, Patras, Greece

10:15

Coffee Break and Exhibition

10:45

Discovery of First in Class, Orally Bioavailable p300/CBP HAT Domain Inhibitors (T04)

Dr Michael MICHAELIDES
ABBVIE, North Chicago, United States

11:30

Novel Bacterial Topoisomerase Inhibitors (NBTI) with Potent Gram-Negative Activity (T05)

Dr Cornelia ZUMBRUNN
IDORSIA PHARMACEUTICALS, Allschwil, Switzerland

12:15

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

12:30

Lunch and Exhibition

13:00

Schrödinger Workshop: Using LiveDesign for Collaborative and Data Driven Drug Design

Session Chair

Dr Malin LEMURELL
ASTRAZENECA, Gothenburg, Sweden

14:00

Catalytic Chirality Generation: New Strategies for Organic Synthesis (T06)

Prof. John BOWER
UNIVERSITY OF BRISTOL, Bristol, United Kingdom

14:45

Nucleophilic Boron for the Synthesis of Functionalized Small Rings (T07)

Prof. Mariola TORTOSA
AUTONOMOUS UNIVERSITY OF MADRID, Madrid, Spain

15:30

A Radical Approach for the Late-Stage Functionalization of Phosphinic Peptides (OC03)

Mr Angelos LELIS
UNIVERSITY OF ATHENS, Athens, Greece

15:45

Coffee Break and Exhibition

16:15

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

16:30

Photoinduced Assembly of C–N Bonds (T08)

Prof. Daniele LEONORI
UNIVERSITY OF MANCHESTER, Manchester, United Kingdom

17:15

Practical Heteroatom- and Group-Transfer Reactions (T09)

Dr Laszlo KURTI
RICE UNIVERSITY, Houston, United States

18:00

Closing of the Day

Session Chair

Prof. Emmanuel MIKROS
UNIVERSITY OF ATHENS, Athens, Greece

08:30

Design and Synthesis of Chemical Probes for Bromodomains (T10)

Prof. Stuart CONWAY
UNIVERSITY OF OXFORD, Oxford, United Kingdom

09:15

A Medicinal Chemist's Perspective on Solute Carriers: Avoiding or Targeting them (T11)

Dr Kim HUARD
GENENTECH, San Francisco, United States

10:00

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

10:15

Coffee Break and Exhibition

10:45

A Chemical Approach to Map Protein Interactions at the Cell Surface (T12)

Dr Erik HETT
MERCK EXPLORATORY SCIENCE CENTER, Boston, United States

11:30

From Fragments to Antibody Drug Conjugates in Emerging Oncology Targeted Therapies (T13)

Dr Laurent SCHIO
SANOFI, Vitry sur Seine, France

12:15

Macrocyclic Modalities for Modulation of Protein-Protein Interactions (OC06)

Dr Stephanie GUERET
ASTRAZENECA MPI SATELLITE UNIT, Dortmund, Germany

12:30

Lunch and Exhibition

13:30

Poster Session 1 (odd numbers)

Session Chair

Dr Gene VAISBERG
CHEMBRIDGE CORPORATION, San Diego, United States

14:30

Awareness of PAINS (Pan Assay Interference Compounds) can Accelerate the Drug Discovery Process (T14)

Prof. Jonathan BAELL
MONASH UNIVERSITY, Parkville, Australia

15:15

Artificial Intelligence in ADMET Modeling and Compound Profiling (T15)

Dr Karl-Heinz BARINGHAUS
SANOFI, Frankfurt, Germany

16:00

Antimicrobial Activity of Curcumin Analog PGV-6, HGV-6 and GVT-6 (OC07)

Dr Leni RITMALENI
GADJAH MADA UNIVERSITY, Yogyakarta, Indonesia

16:15

Coffee Break and Exhibition

16:45

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

17:30

Artificial Intelligence in de Novo Molecular Design (T17)

Dr Ola ENGKVIST
ASTRAZENECA, Mölndal, Sweden

18:15

Closing of the Day

Session Chair

Dr Yves P. AUBERSON
NOVARTIS & EFMC, Basel, Switzerland

08:30

Amides and Chemical Education as Vehicles for Innovation (T18)

Prof. Neil GARG
UNIVERSITY OF CALIFORNIA, Los Angeles, United States

09:15

Discovery of AZD5718, a Novel 5-lipoxygenase Activating Protein (FLAP) Inhibitor (T19)

Dr Malin LEMURELL
ASTRAZENECA, Gothenburg, Sweden

10:00

Discovery of GSK701, a Novel Orally Effective Preclinical Drug Candidate for the Treatment of Malaria (OC08)

Dr Jose Ignacio MARTIN
GSK, Tres Cantos, Spain

10:15

Coffee Break and Exhibition

10:45

Design and Implementation of de Novo Biosynthetic Cascades (T20)

Prof. Sabine FLITSCH
UNIVERSITY OF MANCHESTER, Manchester, United Kingdom

11:30

Catalysis for Total Synthesis (T21)

Prof. Alois FÜRSTNER
MAX PLANCK INSTITUT FUR KOHLENFORSCHUNG, Muelheim an der Ruhr, Germany

12:15

Developing a ‘Reverse-Biomimetic’ Synthesis of Arogenate and its Analogues (OC09)

Ms Louise EAGLING
UNIVERSITY OF BRISTOL, Bristol, United Kingdom

12:30

Lunch and Exhibition

13:30

Poster Session 2 (even numbers)

Session Chair

Prof. Christoforos KOKOTOS
UNIVERSITY OF ATHENS , Athens, Greece

14:30

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

15:15

Prize Ceremony

Dr Yves P. AUBERSON
NOVARTIS & EFMC, Basel, Switzerland

15:20

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

15:35

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

15:50

Coffee Break and Exhibition

16:20

Flow Chemistry and Photochemistry as a Tool for Drug Discovery (T23)

Dr Jesus ALCAZAR
JANSSEN RESEARCH & DEVELOPMENT, Toledo, Spain

17:05

Closing of the Day

20:00

Symposium Banquet

Session Chair

Dr Spiros LIRAS
BIOGEN, Cambridge, United States

08:30

Start Selective and Rigidify: The Discovery Path Towards the Next Generation of EGFR Tyrosine Kinase Inhibitors (T24)

Dr Harald ENGELHARDT
BOEHRINGER-INGELHEIM, Vienna, Austria

09:15

RNA Therapeutics: New Chemical Modalities Becoming a Therapeutic Reality (T25)

Dr Konrad BLEICHER
F.HOFFMANN-LA ROCHE LTD, Basel, Switzerland

10:00

Removable Directing Groups for Late-Stage Functionalisation (OC12)

Dr Miriam O'DUILL
NATIONAL UNIVERSITY OF IRELAND, Galway, Ireland

10:15

Coffee Break and Exhibition

10:45

TLR7/8 Antagonists: from Screening to in vivo Potency (T26)

Dr Claudia BETSCHART
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland

11:30

Allosteric Activation of a Master Metabolic Regulator AMPK: Drug Discovery Opportunities and Challenges (T27)

Dr Kimberly CAMERON
PFIZER, Cambridge, United States

12:15

Closing Remarks & Prize Ceremony

12:30

End of the Symposium