MedChemWatch
Summer Edition July-August 2019

EFMC 50th ANNIVERSARY CELEBRATIONS – WE NEED YOUR HELP!

Next year, 2020, marks the 50th anniversary of EFMC. We have a number of projects planned to mark this milestone, but EFMC wouldn’t have been EFMC for so long without the help and support of the thousands of volunteers and attendees – YOU!

We hope to see you at an EFMC event next year or joining us on social media, and it would be great to hear your thoughts on what you would like to see us doing during the year of celebrations. Please get in touch with your suggestions: Tweet us, post a picture on Instagram, send a message via LinkedIn or Facebook, or even an email at the address below.

We are in the process of compiling and writing a history of EFMC, more of which in the coming months. As part of this, we are collecting pictures that illustrate the first 50 years. If you have photos from EFMC events or EFMC activities, please share them with us. They will add tremendously to the written narrative. We would be very grateful.

Events and EFMC-related activities we would be delighted to hear from you. Please get in touch with us at administration@efmc.info.

EFMC BEST POSTER AWARDEES AT THE EFMC-ACSMEDI MEDCHEM FRONTIERS 2019

EFMC Best Poster Prizes were selected from 107 submissions.

Here is the list of 4 laureates:

• Ms Monika MACIUSZEK
   LIFEARC (United Kingdom)
• Dr Joao SEIXAS
   INSTITUTO DE MEDICINA MOLECULAR (Portugal)
• Prof. Régis MILLET
   UNIVERSITY OF LILLE2 (France)
• Mr Christian STEINEBACH
   UNIVERSITY OF BONN (Germany)

The EFMC Best Poster Prizes consist of a diploma and a 200€ cash-prize – and are awarded at every EFMC Event.

I AM A MEDICINAL CHEMIST/CHEMICAL BIOLOGIST: MEET PEDRO BRANDAO FROM THE UNIVERSITY OF COIMBRA & CQE – UNIVERSITY OF ÉVORA, PORTUGAL

In this edition, we present Pedro Brandao from the University of Coimbra & CQE – University of Évora, Portugal. He believes Green Chemistry associated with Medicinal Chemistry is here to stay, and that chemoinformatics & artificial intelligence will play a major role in assisting future decision-making processes. 

How did you get interested in Medicinal Chemistry?

In high school, I was always very interested in Biology and Chemistry, so when I applied to the University, Pharmaceutical Sciences was my first option. During my MSc in Pharmaceutical Sciences (Faculty of Pharmacy – University of Porto), the curricular units that really caught my attention were Organic Chemistry, Pharmaceutical Chemistry and Drug Design and Synthesis. I felt really fascinated in understanding how drugs could reach and interact with disease targets. For this reason, as an undergraduate student, I joined the Laboratory of Organic and Pharmaceutical Chemistry, and worked under the supervision of Prof. Madalena Pinto in the enantiomeric purity evaluation of new chiral compounds. Furthermore, during the last semester of my MSc (2011), as an Erasmus student, I joined the Laboratory of Organic Chemistry at the University of Urbino “Carlo Bo”, developing work in asymmetric catalysis, under the supervision of Prof. Giovanni Zappia and Prof. Giovanni Piersanti. This was definitely a life-changing experience, which allowed me to further expand my horizons and knowledge, as well as to have a better understanding of the different challenges in Medicinal Chemistry. It also showed me how great it is to share a workplace with a multicultural team, with totally different backgrounds and mindsets, while sharing the same interests. It makes the brainstorming processes much more appealing, at least from my point of view. At this point in life, I decided that Medicinal Chemistry was the field in which I would like to give my contribution to society.

Where and when did you obtain your PhD diploma?

I am currently halfway through my PhD in Chemistry, in the field of Catalysis and Sustainability (CATSUS – Doctoral programme). As a student of this multidisciplinary program, I have three supervisors from three different institutions - University of Coimbra, University of Évora and Instituto Superior Técnico (Lisbon), allowing me to interact with multiple research groups throughout my PhD.

What was the topic of your PhD project?

The topic of my PhD project is the sustainable development of new oxindole derivatives with potential biological activity. My main goal is to develop new molecules with drug-like properties in a “Green by design” way. Oxindole derivatives are very interesting for Medicinal Chemists, with several molecules bearing this structural motif reaching clinical trials and even the market. I intend to develop new “drug candidates” using molecular hybridization and green synthetic procedures, in what concerns solvents, catalytic systems, and activation techniques.

Where do you work at the moment and what is your current position?

I am a PhD student in the CQC/Department of Chemistry – University of Coimbra & CQE – University of Évora, Portugal.

What are your current research interests?
My main focus is the synthesis of new molecules with drug-like properties. I always wanted to develop my work in the area where Medicinal Chemistry meets Green Chemistry, and I am lucky enough to be doing that during my PhD It is challenging and many times makes me think outside the box and explore fields which are out of my comfort zone…and that is exactly the type of challenge I am looking for at this point. Working with privileged structures, I really hope I will be able to find some interesting hit compounds during my PhD. By developing new compounds in a “Green by design” way, I think I will develop a mindset that will have increasingly demanded by industries, regulatory authorities, and academia. Early assessment of pharmacokinetic properties and toxicological features of new drug candidates is also very important to the drug discovery pipeline, and I expect to develop some work in this field as well.

What do you like most in your job?

The constant challenges and the opportunity to learn something new every day.

What kind of tasks your job includes?

At the moment, my main focus is the synthesis, purification and characterization of new compounds. My day-to-day job comprises reaction planning, execution, purification and characterization. Sometimes the results do not appear as quickly as I would expect, so I need to go back to the “drawing board” sometimes and rethink my approach.

What kind of skills your job requires?

Patience, perseverance and grit are mandatory, I would say. When our aim is to do something new, there is always some trial-error involved and sometimes that might turn out to be a little bit daunting. I believe organization skills are also very important to not allow a succession of failures to overwhelm us and to keep us focused in our goals.

What do you consider your biggest achievement in your scientific career?

I hope that moment is still to come. For now, I consider my biggest achievement every time I experience some kind of breakthrough in my lab work, especially when that happens after a succession of failures. It always gives me a very important boost of motivation to further develop my work and explore new tasks.

What are the features of a successful PhD student or postdoc?

As a PhD student, I think it is very important to keep my work well organized and a positive-attitude towards my goals. Despite luck sometimes also emerging as a relevant player during a PhD, a well designed project, combined with a lot of brainstorming and continuous planning are determining factors for a successful PhD.
How would you describe yourself as a supervisor?
Supervision is not one of my tasks as a PhD student. Nevertheless, I really enjoy brainstorming sessions with my supervisors and collaborators in the lab. Therefore, I believe if that time comes, as a supervisor, I will try to develop critical thinking as much as possible since I think that is the only way to achieve real scientific breakthroughs.

What is the most embarrassing thing you did in the lab while doing experiments, e.g. explosions?

Luckily, no explosions so far. Perhaps I am quite “consistent” in my lab work, but so far, I have not experienced any particularly embarrassing moment. However, a few years ago, I had the chance to cooperate in some in vivo assays using Wistar rats. It was great because I really needed to step out of my comfort zone and explore new fields and collaborations, but there were plenty of unusual situations. The most “embarrassing” moment would be perhaps, when we needed to euthanize the first animal. Although I worked multiple times with blood and other tissues, both during my degree and in my professional life as a pharmacist, everyone said I got really pale during that process…After the first animal, everything went smoothly as expected and desired.

Which scientist do you admire the most and why?

This is a very difficult question. I think it is very important to get inspired by those who work directly with you. Therefore, the supervisors I have today and I had in the past, my lab coworkers (and I already worked in multiple locations, so it is plenty of them), I somehow admire all of them, since they helped me to become the “scientist” I am today and to determine which kind of scientist I want to become in the future. Some by the passion they have for the field, others by their work ethics, others by their great knowledge transfer skills. Some by even allowing me to have a voice in the development of projects and to take part in some decision-making processes. Others, by simply showing me the kind of scientist I do not want to become.
In a totally different note, there is a scientist that, even though our fields barely overlap, whose approach to Science, and the way he addresses several (I would say) delicate topics in the scientific community are simply inspiring. He is Dr. John Tregoning, from the Department of Medicine – Imperial College London. He writes a blog about academic careers and already wrote opinion articles in several publications. I keep many of those in a folder with the title “motivation” in my laptop. If I would have to choose one of the articles which inspired me the most, I would say it was “No researcher is too junior to fix science” (Nature, 2017, vol. 545, 7), which I believe should be mandatory reading for any young scientist and first year’s PhD students.

Did you experience any unfair situations during your scientific career?

Unfortunately, I have experienced some unfair situations, but I always try to convert those unwanted situations into opportunities. Grit is definitely one of the most important characteristics of a scientist, and those situations helped me to understand the importance of perseverance and the passion I have for the field of Medicinal Chemistry. They helped me to develop healthy and strong work ethic, as well as to develop a good network of contacts.

Which paper of yours you are the proudest of and why?

I would say it is always the last one I publish. Nevertheless, I really enjoy writing review papers. The ones I had the chance to write so far, really allowed me to dwell into a certain topic and that is always how I learn the most about something. It is a great way to know what has been done and how, and it also can show us some opportunities on what there is still to be done in a certain field. It is also a great opportunity to cooperate with different scientists. Anyway, feel free to take a look in my google scholar or my researchgate profile.

Which field of medicinal chemistry do you consider the most promising in the future?

Well, I believe Green Chemistry associated with Medicinal Chemistry is here to stay. I think regulatory authorities will start to demand the application of the twelve principles as much as possible in both industries and R&D units. The depletion of resources, environmental concerns, and health hazards, will cause a shift in the way many sciences are performed, including Medicinal Chemistry. There will be less and less room for trial-error and a great deal of planning will be required. For that, I think chemoinformatics, as well as artificial intelligence, will play a major role in assisting in decision-making processes. Regarding the disease targets, I think the number of publications concerning new antibiotic drug candidates will increase dramatically, as the failure of current therapeutic options will become more evident due to resistance mechanisms. Ageing and chronic diseases are also topics that will continue to expand due to demographic and social pressure. In diseases such as cancer and other diseases in which the immune system plays a pivotal role, I think biological drugs might become first-line therapy in multiple diseases and overcome the use of small-molecules.

Want more? Read all the interviews here!

EFMC PHOTO COMPETITION 2019: CAST YOUR VOTE BEFORE AUGUST 10!

Your votes will choose the top 20 shots out of the 64 submissions we received!

The selected pictures will be displayed at the upcoming EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry (EFMC-ASMC’19) for the attendees to vote and choose the grand winner and two most-meritorious runners-up.

Vote now!

MISSED THE JMMC 2019? READ THE REPORT

The 11th year of the international symposium "Joint Meeting on Medicinal Chemistry" (JMMC) took place in Prague, Czech Republic, at the Pyramida Hotel from Thursday June 27 to Sunday June 30, 2019. The meeting of pharmaceutical chemists was organized on the occasion of the 50th anniversary of the Faculty of Pharmacy in Hradec Kralové by the Section of synthetic drugs of CzMA (Czech Medical Association of J. E. Purkyn''.chr('283').'') and IOCB CAS (Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences) under the auspices of the European Federation for Medicinal Chemistry in collaboration with the company Guarant s.r.o..

This year's JMMC conference was a continuation of more than twenty years tradition of scientific meetings taking place every two years. More than 150 pharmaceutical chemists from 17 European countries, as well as Turkey, Taiwan, Japan, South Korea, Canada and the USA, listened to 9 plenary, 16 key lectures and 7 short presentations. A great promise for the future was the high participation of students. An important part of the conference were the discussions relating to the 94 posters. Attention was paid to advances in drug development in major therapeutic areas, especially new drugs in the antiviral, antineoplastic, Alzheimer's disease treatment, new anti-inflammatory, antiprotozoal molecules, and/or newly developed antibacterial active compounds. The greatest attention among the participants was appropriately devoted to the invited plenary lecture by Dr. Tomáš Cihlá''.chr('345').'', Vice President for Virology at Gilead Sciences, San Francisco Bay Area, USA, who presented to conference participants the new Remdesivir drug being developed against Ebola: Discovery and Development of Antiviral Therapeutics for Emerging and Neglected Viral Infections.

The Faculty of Pharmacy of Charles University was represented in an exemplary manner not only by the Dean prof. Tomáš Šim''.chr('367').''nek, who welcomed the participants on Thursday afternoon, June 27, but also members of the Preparatory Committee (Prof. Vinšová, Prof. Doležal, Doc. Krátký, Dr. Ku''.chr('269').''erová, Dr. Zitko) and other active participants from the Department of Pharmaceutical Chemistry and Pharmaceutical analysis and the Department of Organic and Bioorganic Chemistry. The organizers succeeded to organize a pleasant entertainment program, such as the performances of the student jazz group DiJazzTivy, or a social evening at the Monastery Great Restaurant at Strahov.

We also thank the event sponsors: Advion Ltd., Interchim, Bentham Science, ChemPubSoc Europe, ''.chr('268').''CHS, IOCB Tech and the EFSA-CDN project, without whose support it would not be possible to organize this international symposium. We cannot overlook and must acclaim the professional support of Guarant, s.r.o. All the participants left for their homes very satisfied, gained a lot of valuable information and established new scientific contacts. The next meeting of pharmaceutical chemists JMMC will be hosted by Bratislava, Slovakia, in June 2021.

Report by: Prof. RNDr. Jarmila Vinšová, CSc. and Prof. Pharm Dr. Martin Doležal, Ph.D.

UPCOMING EFMC SPONSORED EVENTS

The EFMC invites you to have a look at the following events:

Twenty Years of the Rule of Five
20th November, 2019 | Nottingham, United Kingdom

It has been over twenty years since Lipinski published his work determining the properties of drug molecules associated with good solubility and permeability. Since then, there have been a number of additions and expansions to these “rules”. There has also been keen interest in the application of these guidelines in the drug discovery process and how these apply to new emerging chemical structures such as macrocycles.
This symposium will bring together researchers from a number of different areas of drug discovery and will provide a historical overview of the use of Lipinski’s rules, as well as looking to the future and how we use these rules in the changing drug compound landscape.

Features of the Meeting

• Historical look at the use of the Rule of Five
• New parameters used in drug discovery
• Look forward to the next 20 years
• Panel discussions in each session
• Plenary speakers, poster session, and drinks reception

Deadlines:
Poster Abstract deadline: 8th October
Standard registration deadline: 18th October
For more information please contact: maggi@maggichurchouseevents.co.uk

MedChem2019 - Peptide Drug Discovery: A Niche Area?
22nd November 2019 | Brussels, Belgium

This year, the symposium will delve into the developments in the therapeutic use of peptides.

Confirmed Speakers

• Linkers for Peptide Conjugation
   Prof. Fernando ALBERICIO
   UNIVERSITY OF KWAZULU-NATAL, Durban, South Africa

• Synthetic Immune System Engagers – a Peptide-based Approach to Immune-oncology
   Prof. Christian F.W. BECKER
   UNIVERSITY OF VIENNA, Wien, Austria

• Macrocyclization as an Enabling Tool Toward Novel Peptide Drug Candidates
   Prof. Eric MARSAULT
   UNIVERSITY OF SHERBROOKE, Sherbrooke, PQ, Canada

• Targeting Receptor Complexes: A New Dimension in Drug Discovery
   Prof. Kristian STROMGAARD
   UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark

• Gate2Brain, Opening the Gate to CNS Therapies
   Dr Meritxell TEIXIDO
   INSTITUTE FOR RESEARCH IN BIOMEDICINE, Barcelona, Spain

Deadlines:
Poster submission & early-bird fee: 10th October

For more information, please visit: www.medchem.be
Share the word on social media using the #MedChem2019

NEWS OF THE FRENCH SOCIETY OF MEDICINAL CHEMISTRY (SCT)

The SCT is pleased to announce its upcoming one-day thematic symposium: “Drug Discovery in the RNA world” – scheduled to take place on December 11th, 2019 in Paris, France. The 4th one-day thematic symposium will be focusing on the contribution of Chemical Biology to Molecular Therapeutic Innovations.

The aim of the symposium is to illustrate the great potential and applications of RNA-targeting modalities in contributing to therapeutic innovation. This meeting is dedicated to a large audience of organic and medicinal chemists, biochemists and biologists from academic and industry. During this day, we will focus on recent advances in the field of RNA targeting using small molecules as well as oligonucleotides: the synthetic challenges involved in the design of RNA-targeting agents and on the validation of relevant RNA targets, as well as on the current methodologies used to study RNA/ligands interactions. RNA has already been drugged. Ribosomal RNA was drugged serendipitously with natural product antibiotics and later linezolid. A design-driven approach to drugging RNA was achieved with antisense oligonucleotides (ASOs) and then by RNA interference (RNAi) mechanisms.

More recently, small molecules that bind to the FMN riboswitch and to SMN2 pre-mRNA were reported and are close to clinical application. All those recent developments in the field of RNA-targeting definitely hold promise for future therapeutic applications.

List of confirmed speakers:

Matthew DISNEY (Scripps, Florida, USA): “Translating RNA sequence into lead small molecule medicines.”
Maria DUCA (Université Côte d’Azur, France): “Synthetic small-molecule RNA ligands : Scope and applications”
Mélanie ETHEVE-QUELQUEJEU (Université de Paris, France): “Modified RNAs as Molecular Tools for Structural and Functional Studies of RNAs dependents Enzymes”
Eric ENNIFAR (Université de Strasbourg, France): "Structure-guided discovery of novel ligands targeting the HIV-1 genomic viral RNA"
Jonathan HALL (ETH Zurich, Switzerland): “A Bright Future for Oligonucleotide Drugs”
Gerhard MUELLER (Gotham Therapeutics, Germany): “Epitranscriptomic readers, writers, and erasers: a biophysics and medicinal chemistry perspective”
Alleyn PLOWRIGHT (Sanofi-Aventis Deutschland GmbH, Germany): “Modulating RNA - recent drug discovery approaches and opportunities for diverse modalities”
Helene TRAN (Servier Research Institute, France): “Antisense Oligonucleotides Therapeutics for CNS Disorders”

Link for registration:
http://www.sct-asso.fr/fall_one_day_symposium.html

NEWS FROM THE BIOLOGICAL AND MEDICINAL CHEMISTRY SECTOR (BMCS) OF THE ROYAL SOCIETY OF CHEMISTRY (RSC)

The BMCS is pleased to announce the call for nominations for the BMCS Hall of Fame & the Capps Green Zomaya Memorial Awards 2020, and some upcoming events.  

BMCS HALL OF FAME: CALL FOR NOMINATIONS
The BMCS Hall of Fame aims to recognize prominent chemists for outstanding, sustained, contributions to any area of interest to the BMCS. This is an Individual award to recognize prominence and significant, sustained, scientific impact in the field of medicinal chemistry, agriscience or chemical biology, including teaching excellence, outstanding contributions to the BMCS, or any combination thereof.
NB This award is open to nominees resident in the UK and continental Europe
Process
Independent nominations should include a one page synopsis detailing the justification and the candidate’s CV & publication list. The nomination may be further bolstered by additional independent letters of support
Nominations should be submitted by the end of September 2019
For more information go to https://www.rsc.org/Membership/Networking/InterestGroups/BMCS/Activities/HallofFame.asp


CAPPS GREEN ZOMAYA MEMORIAL AWARD 2020: CALL FOR NOMINATIONS
The Biological and Medicinal Chemistry Sector of the Royal Society of Chemistry is pleased to invite nominations for the ninth Capps Green Zomaya Memorial Award in medicinal or computational chemistry
The Award will be given to the individual judged to have made an important contribution to the discovery or development of new medicines. Nominations are invited for candidates, up to the age of 40, working in UK or international laboratories (candidates over the age of 40, who have taken career breaks, will be considered)
A Royal Society of Chemistry commemorative medal and certificate will be awarded to accompany the prize of £2,000
NB This award is open to nominees resident anywhere in the world
Nominations should be submitted no later than 31st October 2019 to: Maggi Churchouse, RSC-BMCS Secretariat: E-mail: maggi@maggichurchouseevents.co.uk
For further details, please access the activities link on www.rsc.org/bmcs


2nd RSC BMCS/ RSC CICAG ARTIFICIAL INTELLIGENCE IN CHEMISTRY SYMPOSIUM
2nd to 3rd September 2019, Fitzwilliam College, Cambridge, UK
Website: http://www.rsc.org/events/detail/38130/2nd-rsc-bmcs-rsc-cicag-artificial-intelligence-in-chemistry
Synopsis: AI is experiencing a renaissance in development of new methods and practical applications to ongoing challenges in chemistry. This two-day conference will present the current efforts in applying these new methods. We will combine aspects of artificial intelligence and deep machine learning methods to applications in chemistry, agriscience, bioorganic chemistry, and chemical biology


20th RSC / SCI CAMBRIDGE MEDCHEM SYMPOSIUM
8th to 11th September, Churchill College, Cambridge, UK
Website: http://www.rsc.org/events/detail/35363/20th-sci-rsc-medicinal-chemistry-symposium
Synopsis: The 20th symposium, Europe’s premier biennial Medicinal Chemistry event, focussing on first disclosures and new strategies in Medicinal Chemistry. This conference will be of interest to both academic and industrial scientists engaged in all aspects of the drug discovery and development process.


20 YEARS OF THE RULE-OF-FIVE SYMPOSIUM
20th November 2019, Sygnature Discovery, Nottingham, UK
The call for poster abstracts will close on 6th October
Website: http://www.rsc.org/events/detail/39112/twenty-years-of-the-rule-of-five
Synopsis: This symposium will bring together researchers from a number of different areas of drug discovery and will provide a historical overview of the use of Lipinski’s rules, as well as looking to the future and how we use these rules in the changing drug compound landscape

THIS MONTH’S HIGHLIGHTED MEDCHEMCOMM ARTICLE IS:

"Glycans in Drug Discovery"

Jesús Jiménez-Barbero, Ana Gimeno et al. from CIC bioGUNE discuss the recent advances in the design of glycomimetics, glycan-based vaccines and therapeutics and highlight the potential of carbohydrates in drug discovery.

Glycans are key players in many biological processes. They are essential for protein folding and stability and act as recognition elements in cell–cell and cell–matrix interactions. Thus, being at the heart of medically relevant biological processes, glycans have come onto the scene and are considered hot spots for biomedical intervention. The progress in biophysical techniques allowing access to an increasing molecular and structural understanding of these processes has led to the development of effective therapeutics. Indeed, strategies aimed at designing glycomimetics able to block specific lectin–carbohydrate interactions, carbohydrate-based vaccines mimicking self- and non-self-antigens as well as the exploitation of the therapeutic potential of glycosylated antibodies are being pursued. In this mini-review the most prominent contributions concerning recurrent diseases are highlighted, including bacterial and viral infections, cancer or immune-related pathologies, which certainly show the great promise of carbohydrates in drug discovery.

 

Read the article!

THE LATEST EDITION OF MEDCHEMCOMM, THE OFFICIAL JOURNAL OF THE EFMC, IS AVAILABLE AT:

MedChemComm

 

EFMC SPONSORED EVENTS

November 20, 2019 
Nottingham, United Kingdom
Twenty Years of the Rule of Five Symposium

November 22, 2019 
Brussels, Belgium
MedChem 2019 - Peptide Drug Discovery: a Niche Area?

EFMC ORGANISED EVENTS

September 1-5, 2019 
Athens, Greece
EFMC-ASMC'19: EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry

September 5-6, 2019 
Athens, Greece
EFMC-YMCS 2019: 6th EFMC Young Medicinal Chemist Symposium

September 6-10, 2020 
Basel, Switzerland
EFMC-ISMC 2020: XXVI EFMC International Symposium on Medicinal Chemistry

EFMC SPONSORED SCHOOLS

September 11-13, 2019 
Pescara, Italy
Summer School in Pharmaceutical Analysis (SSPA)

September 15-20, 2019 
Vienna, Austria
EUROPIN Summer School on Drug Design

JOB PORTAL

Tenure-Track Professorship for the field of Pharmaceutical Neurochemistry, University of Vienna, Department of Pharmaceutical Chemistry, Vienna, Austria

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Tenure-Track Professorship "Medicinal Chemistry of Chemotherapeutics", University of Vienna, Department of Pharmaceutical Chemistry, Vienna, Austria

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PhD position, Université Côte d'Azur, Chemistry Institute, Nice, France

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PhD/Post Doc positions at Université de Montréal (NSERC-Servier Research Chair in Medicinal Chemistry and Chemical Biology), University of Montreal, Chemistry, Montreal, Canada

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