Monthly Newsletter November 2021


To acknowledge outstanding achievements in the field of Medicinal Chemistry and Chemical Biology, EFMC presents three awards every two years. The 2022 Awards will be presented at the XXVII EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2022) to be held in Nice, France on September 4-8, 2022.

All 3 awards consist of a diploma, 7.500€ and an invitation to give a headline presentation at EFMC-ISMC 2022.

Deadline for submission: January 31, 2022

The Award will be given for outstanding achievements in scientific research including contributions to the development of international organisational structures in Medicinal Chemistry and Chemical Biology.

To acknowledge and recognise outstanding research in the field of Medicinal Chemistry in its broadest sense by a young scientist. This Award has been established with the support of UCB Pharma.

To encourage innovation and investigation in technological development related to drug discovery, this Award, established with the support of the Prous Institute, will be given for the discovery, evaluation, or use of new technologies.

Nominations for these Awards should consist of a nomination letter, a brief CV including a list of selected publications, and two supporting letters. Self-nominations are accepted. The nominations should be submitted to Prof. Rui Moreira, President of the EFMC, via the following link:


To acknowledge and recognise outstanding young medicinal chemists and chemical biologists (≤ 12 years after PhD) working in European industry and academia, the EFMC established the "EFMC Prize for a Young Medicinal Chemist or Chemical Biologist in Industry" and the "EFMC Prize for a Young Medicinal Chemist or Chemical Biologist in Academia".

These two prizes are given annually and consist of a diploma1.000€ and an invitation for a short presentation at an EFMC symposium.

The prize-winners will be invited to give lectures at the XXVII EFMC "International Symposium on Medicinal Chemistry" (EFMC-ISMC 2022).

Deadline for nominations is January 31, 2022.

EFMC Prize for a Young Medicinal Chemist or Chemical Biologist in Industry

Nominations should be written by the candidate’s supervisor and consist of:

  • a letter by the supervisor.
  • a brief CV of the candidate.
  • an abstract of the potential oral presentation.

EFMC Prize for a Young Medicinal Chemist or Chemical Biologist in Academia

Applications should consist of:

  • a one-page letter by the candidate, including a short rationale for their application.
  • one page with the five key publications.
  • a brief CV of the candidate.
  • an abstract of the potential oral presentation.


The “literature spotlight” section of the newsletter will bring you a summary of the recently published research in a concise and accessible way. Multiple thematics from different journals will be highlighted thanks to the valuable contribution of members of the communication team.

This contribution will focus on the recently published article on “In-Cell Generation of Anticancer Phenanthridine Through Bioorthogonal Cyclization in Antitumor Prodrug Development” (by H. Maslah et al. in Angew. Chem. Int. Ed.).

Achieving selectivity for cancer vs healthy cells is one of the biggest challenges in oncology drug discovery. Many cytotoxic drugs cause toxicity to both cancerous and healthy cells, thus leading to side-effects in patients during treatment, and limiting the therapeutic window.

The use of prodrugs is a promising approach to increase the tumour activity of such drugs while decreasing deleterious side-effects in other tissues. The strategy consists of using activity-masked molecules, that is, bioactive molecules covalently linked to a moiety that renders them inactive. The active molecule is then released in the tumour through an enzymatic and/or other chemical transformation thus exploiting the distinct metabolism of cancer cells. For instance, commonly used prodrugs take advantage of the higher levels of reactive oxygen species (ROS), hypoxia, and lower pH in tumours, or the overexpression of certain enzymes.

One limitation of this strategy is that the prodrugs can often still bind the biological target to a certain extent. To circumvent this limitation, Maslah et al. have recently reported an alternative prodrug strategy wherein, instead of using a promoiety, the bioactive molecule is released after intramolecular cyclisation of a precursor. They chose a phenanthridine derivative with a large and planar structure (ToxPhen) as the cytotoxic drug; the prodrug itself was a ring-opened precursor protected with a boronic acid (ProToxPhen). The intention is that the high ROS levels in cancer cells would oxidise the vinyl boronic acid to an enol group, which would tautomerise into its keto form before reacting with an aniline to generate the phenanthridine scaffold. They first evaluated the feasibility of the approach with a simple model system and were able to detect precursor cyclisation triggered by hydrogen peroxide with 1H NMR spectroscopy and fluorescence spectrometry. This cyclisation occurred at extremely fast rates. In KB (epidermal carcinoma) cancer cells, treatment with ProToxPhen only reduced cell viability upon addition of peroxynitrite, that mimics the oxidising environment of the tumour. The authors ascribe the high difference in bioactivity between ToxPhen and its prodrug to their high structural differences (completely planar vs twisted biaryl). They also found the activation-cyclisation process to be even faster than in the hydrogen peroxide experiment. Such fast rates are optimal for this application, as otherwise the active molecule would start diffusing out of the tumour before full release, thus requiring higher concentrations.

All in all, this paper proposes a new prodrug strategy based on “cyclisation-in-cell” precursors with high rates and high selectivity for cancer cells, which will surely soon be expanded to structurally different drugs and chemical triggers, and other applications such as imaging.

Maslah, H.; Skarbek, C.; Gourson, C.; Plamont, M.; Pethe, S.; Jullien, L.; Le Saux, T.; Labruère, R. In''.chr('8208').''Cell Generation of Anticancer Phenanthridine Through Bioorthogonal Cyclization in Antitumor Prodrug Development. Angew. Chemie Int. Ed. 2021, 60, 24043–24047, doi:10.1002/anie.202110041.


The EFMC Communication Team is actively preparing for the Holiday Season and invites you all to contribute to its Social Media Advent Calendar.

As of December 1st, please share the most festive picture from your lab with us and get showcased on the EFMC Twitter or Instagram account. The most-liked picture by December 24th noon CET will win a 25€ prize and an EFMC GoodieBox.

How to participate?

  • Share your picture by PM via Twitter, or
  • Tag us from a public account on Twitter (@EuroMedChem) or Instagram (@euromedchem), or
  • Share your picture and details via email to


In this edition, our #Iamamedicinalchemist is the runner-up of the 2021 EFMC Prize for Young Medicinal Chemist or Chemical Biologist in Academia: Markus Muttenthaler from the University of Vienna, Austria.

Get to know him better by reading our interview below.

Where and when did you obtain your PhD diploma?

I obtained my PhD in Biological and Medicinal Chemistry in 2009 from the University of Queensland, Brisbane, Australia.

What was the topic of your PhD project?

Peptide Engineering – Controlling the folding of disulfide-rich peptides. My PhD focussed on developing new methodologies to accelerate the discovery and characterisation of bioactive peptides from animal venoms. Such venom peptides are valuable molecular probes and promising therapeutic leads due to their exquisite potency and selectivity.

Where did you have your postdoc position?

2009-2011: in the laboratory of Prof. Paul Alewood (venom peptide drug discovery) at the Institute for Molecular Bioscience, at the University of Queensland, Brisbane, Australia.
2011-2013: as a Marie Curie Fellow in the laboratory of Prof. Philip Dawson (inventor of native chemical ligation) at the Scripps Research Institute in La Jolla, California.
2013-2015: as a Marie Curie Fellow in the laboratory of Prof. Fernando Albericio (peptide chemistry) at the Institute for Biomedical Research, Barcelona, Spain.

Where are you currently working and what is your current position?

I am an Associate Professor and lead two research laboratories, one at the Institute of Biological Chemistry at the University of Vienna, Austria, and one at the Institute for Molecular Bioscience at the University of Queensland, Australia.

What are your current research interests?

My research interests are centred around neuropeptides and natural product drug discovery with a particular focus on bioactive peptides derived from animal venoms. We take advantage of these vast natural peptide libraries to identify new molecular probes and therapeutic leads for the study and treatment of neuropathic pain, gastrointestinal disorders, breast cancer and autism.

How would you explain what your research area is to non-scientists?

We investigate how diseases work and develop therapeutic strategies to treat them.

What do you like best about your work?

The intriguing links between nature, chemistry, biology and medicine.

What kind of tasks does your work involve?

Going on field trips, collecting venom, discovering and synthesising new bioactive compounds, understanding their interactions with human physiology, and developing drug candidates to improve human health.

What kind of skills does your work require?

Scientifically: a good understanding of chemistry, pharmacology, biology
Equally important: perseverance, curiosity, optimism, and a good team to work with.

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

Still in the making, but it is already great to be finally in a position where I can pursue and translate several of my ideas. The next few years will be highly interesting to see if these new approaches also pan out!

Which of your papers are you most proud of and why?

There are several publications that come to my mind for different reasons, but two are certainly special to me: my first JACS paper: Solving the α-conotoxin folding problem: efficient selenium-directed on-resin generation of more potent and stable nicotinic acetylcholine receptor antagonists –– as it describes key aspects of my PhD work and provided me with confidence that I can produce innovative and high quality of work; and our latest Nature Reviews Drug Discovery Review, Trends in Peptide Drug Discovery – as it provides an in-depth overview of the field I work in covering the peptide drug discovery and development landscape from its beginning to its future.

How many PhD students and postdocs do you currently supervise? Are you currently looking for a new PhD student or a postdoc?

11 postdocs and 6 PhD students. Yes, I am always looking for talented people with the right background and passion.

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

I would be lying if hard-working wouldn’t be part of the top three. Cutting-edge research is highly challenging and a strong science education with well-developed laboratory skills is necessary to start tackling significant challenges. A positive can-do-attitude coupled to independent and innovative thinking is also very important.

How would you describe yourself as a supervisor?

Supportive, facilitating, with high expectations. I like to see people succeed.

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

Yes, I did blow up a fumehood …. luckily no-one got hurt.

What are your recommendations for a book, podcast, website, blog, YouTube channel or film?

Book: Perfume, by Patrick Süskind
Movie: Memento
Blog: In the pipeline

Which scientist do you admire the most and why?

Stephen Kent – highly innovative and advanced our field in many new directions.

Have you experienced any unfair situations during your scientific career?

I am sure I have – the trick is to forget them fast and not let them get to you – there are always bigger and more important things to focus on.

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

Peptides of course ;) I don’t think there is one specific field that stands out, it's the diversity and complementary nature of many approaches and technologies that counts.

What advice would you give to someone who wants to know more about your field?

A good place to start would be our review: Trends in peptide drug discovery. Nature Reviews Drug Discovery; take some online Medicinal Chemistry or Chemical Biology lectures.

What would you like to ask from other medicinal chemists?

Keep up the good work!

What would you expect to be the next major breakthrough in medicinal chemistry?

That’s a tough one – I think more advanced drug delivery technologies will play an important role as this remains a limiting step for many otherwise promising therapeutic approaches.


In lieu of an interview in the October edition, let us offer you the chance to meet another #Iamamedicinalchemist: Riccardo Martini from Discngine, France.

Get to know him better by reading our interview below.

Where and when did you obtain your PhD diploma?

I obtained my PhD in “Chemical and Pharmaceutical Sciences” at the University of Siena, Italy in the group of Professor Maurizio Botta. It was the beginning of 2017.

Where are you currently working and what is your current position?

I am currently working for the French company Discngine, in Paris. Discngine develops and provides state-of-the-art IT solutions, mainly for customers involved in life science R&D.

The title of my position is “Senior Consultant”, which, even if it does not seem to tell much, is a pretty good description of what my duties are- helping our customers with, well, a little bit of everything!

What do you like best about your work?

There are multiple aspects I love about my work. For starters, it is never boring! I have the possibility to help our customers in many different areas: from designing a custom solution to handling the administration of an application, to give training on various software, to provide scientific and technical support, to suggest and implement new ways for integration and automation… as I said – a bit of everything.

Another aspect I really like about my job is that it gives me the possibility to interact with many smart and talented people, both co-workers and customers. This often results in producing enriching experiences, allowing me to continuously grow.

Finally, it is really rewarding when I see a customer heavily relying on a piece of work I have done, or helped with. It really shows how much important what we do is.

What kind of tasks does your work involve?

See the previous answer for some examples. More in general, the kind of tasks my work involves are all around the ideation, design, implementation, management, and maintenance of custom IT solutions deployed at customers’ sites. All of this without forgetting the “human factors” as engagement and support of the user community.

What kind of skills does your work require?

My work requires a broad range of competencies. Of course, there is the need for a solid scientific and technical base, but that’s not all. Particularly important skills are also in presentation, project management and people management. It is important to have the capability to quickly grasp - and keep in mind - the “big picture”, so that one can better proceed with all the steps I have mentioned in the previous answer. Mental elasticity is finally crucial; not only is the fundamental to understand the needs, but also what is required to adapt a project when it has already started. In a real-world scenario, we need to be prepared to navigate through an ever-changing landscape of possibilities. Be able to steer in time is the key between success and failure.

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

That depends on what one intends with “successful”. Success and sense of achievement are strictly personal feelings. Therefore, my answer here is based purely on my personal idea of success – which, in the case of a PhD student or postdoc, is to put themselves in the best conditions to proceed towards what they would like to do with their next steps. Based on such premise, I would say that to be successful they should be able to not think only about science. They should be able to think about their career path, to create opportunities for themselves, to not waste any occasion to interact with other scientists as well as not-scientists. So, translated into feature, I think that I could say: “communicative planner”.

How would you describe yourself as a supervisor?

I think that many of the ex-students I supervised while working at the university would agree on these 3 words: “tough but fair”. I believe it fits.

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

The usage of AI-assisted computational methods to reliably predict 3D protein structures.


The MedChem Division of the German Chemical Society (GDCh) would like to invite you to the next #MedChemCASES online seminar which will be held on November 18 by Keith Graham.

The topic of the webinar will be “Discovery of potent SOS1 inhibitors and their pharmacological investigations to disrupt the RAS-SOS1 interaction”

In addition, the NextGenMedChem group of GDCh and the Young Scientists Network of the EFMC will take the opportunity of the event to host a round table discussion on the topic “Life as a foreign scientist in Germany” where panellists from various origins will tackle topics such as moving to, working, and living in Germany.

Case Study

Mutants of RAS are major oncogenes and are prevalent in many human cancers, however efforts to develop drugs that directly inhibit the corresponding constitutively active RAS proteins have been unsuccessful so far, although there are promising new findings for KRas-G12C covalent inhibitors. We focused on SOS1, the guanine nucleotide exchange factor (GEF), and an activator of RAS. We identified good starting points for medicinal chemistry activities using both high-throughput and fragment screens. Initial optimizations resulted in the discovery of the first nanomolar SOS1 inhibitors, which effectively downregulated active RAS in tumour cells. Here, the key findings on our path to identifying novel potent and cellular active small molecule inhibitors will be described. These inhibitors efficiently disrupted the interaction between KRAS and its exchange factor SOS1, this mode of action was confirmed by a series of biophysical techniques. The binding sites, mode of action and selectivity were elucidated using crystal structures of KRASG12C–SOS1, SOS1 and SOS2. By preventing formation of the KRAS–SOS1 complex, these inhibitors block the reloading of KRAS with GTP and, therefore, showed antiproliferative activity. Our probe BAY-293 selectively inhibited the KRAS–SOS1 interaction with an IC50 of 21 nM and is a valuable chemical probe for further investigations. In cells with wild-type KRAS the complete inhibition of the RAS–RAF–MEK–ERK pathway was observed. In a mutant KRAS cell line, SOS1 inhibition resulted in a reduction of pERK activity by 50%. Together, the data indicate that inhibition of GEFs may represent a new viable approach for targeting RAS-driven tumours.

Round Table Discussion

Join our panel of various scientists to hear about their experience as foreigner. Ask questions and learn the tips & tricks to succeed in moving to, working, and living in Germany.

  • Eleonora Diamanti (Helmholtz Institute for Pharmaceutical Research Saarland, Germany)
  • Louise Eagling (Nuvisan, Germany)
  • Dr Keith Graham (Boehringer Ingelheim, Germany) 
  • Katarina Iric (DyNAbind, Germany)
  • Andrea Unzue-Lopez (Merck, Germany)

Register for free here: Webinar Registration - Zoom

#GDCh (MedChem Division), #NextGenMedChem.


After the worldwide situation, the Spanish Society of Medicinal Chemistry (SEQT) decided that the XIII Workshop of the SEQT would be held as a fully face-to-face event, from October 20 to 22, in the city of Albacete, Spain. In order to create a safe environment, together with the usual actions during the event, all attendees presented their vaccination certificate and negative antigen test 24 hours before their trip.

From the scientific point of view, the event had two clearly differentiated parts: Light in Therapies, which focused on topics such as drug delivery with light, photosensitizers and photodynamic therapies, photopharmacology, etc. and New Therapies, such as CAR-T, CRISPR or PROTAC technologies. Focusing on the central role of chemistry at the interfaces with biology, biochemistry and medical sciences. The scientific level reached was very high, giving all participants the opportunity to listen to speakers presenting the latest advances and to openly discuss with the medicinal chemistry and chemical biology international community.



The SCT, the SFM (French Society of Microbiology), and sponsors invite you to an exciting two-day symposium on December 9-10, 2021 entitled: On the hunt for next generation antimicrobial agents.

This symposium will bring together some of the most influential researchers involved in these endeavors and will be of interest to a wide audience of scientists, medicinal chemists, doctors, and microbiologists.

The rapid emergence of antibiotic resistance (AMR) in bacteria is one of the most pressing global health threats. Despite its significance, the potential impact of this phenomenon remains largely underappreciated by a large portion of the population. The recent Covid-19 pandemic has further intensified the use of antibiotics, often without clinical justification, which is expected to further impact on future AMR statistics. In Europe alone, >33,000 deaths per year are attributable to resistant infections (700,000 world-wide), resulting in a substantial clinical and financial burden on healthcare providers, clinicians, patients, and patients’ families. The cost associated with the management of these infections is estimated at $ 11.3 billion. If we do not strengthen our efforts to stem the tide of antimicrobial resistance, it is predicted that by 2050 antibiotic resistant infections may cause 10 million deaths worldwide.

Fortunately, many academic groups and a small number of biotech companies, have chosen to take up the exciting challenge of replenishing the antibiotic development pipeline with innovative molecules. Experts in drug discovery and microbiology will talk about their recent advances in presentations targeting a multidisciplinary audience.

Confirmed speakers

  • Dr Florence Séjourné, Beam Alliance, France
  • Dr Giulia Manina, Institut Pasteur Paris, France
  • Prof. Paul Hergenrother, University of Illinois, United States
  • Dr Glenn Dale, Bioversys, Basel, Switzerland
  • Dr Robert Bates, GSK, Tres Cantos, Spain
  • Prof. Klass Martinus Pos, Goethe University Frankfurt, Germany
  • Dr Tim Opperman, Microbiotix, Massachusetts, United States
  • Dr Kevin Pethe, Nanyang Technological University, Singapour
  • Dr Cédric Couturier, Evotec, France
  • Prof. Paul Race, Bristol University, United Kingdom
  • Prof. Michel Arthur, Centre de Recherche des Cordeliers, Paris
  • Dr David Davies, Antabio, France
  • Dr Garrett Moraski, Montana State University, United States

Registration fee: 25€
Website: click here
Registration link: click here


The BMCS is pleased to announces some upcoming events:

  • 3rd RSC/SCI Symposium on Antimicrobial Drug Discovery
  • 5th RSC/DMDG/DMG New Perspectives in DMPK (Abstract deadline is November 25th) 
  • 8th RSC-BMCS Fragment-Based Drug Discovery Meeting

VIRTUAL - 3rd RSC / SCI Symposium on Antimicrobial Drug Discovery

15th and 16th November 2021

Last chance to register


Synopsis:  Coinciding with WHO’s World Antibiotics Awareness week, this two-day meeting will examine the latest advances in antimicrobial drug discovery from a medicinal chemist’s perspective, focusing on the particular challenges associated with developing antimicrobials whilst also showcasing emerging strategies for tackling infection.


5th RSC / DMDG / DMG New Perspectives in DMPK   

22nd and 23rd February 2022, Liverpool, UK

The call for abstracts will close on 25th November (oral) and 13th January 2022 (oral)


Synopsis:    Members from across the DMPK research community are encouraged to join colleagues from across academic, industrial, and third-sector institutions and contribute to the ongoing discussion, evolution and application of DMPK in various scenarios.


Fragments VIII:  8th RSC-BMCS Fragment-based Drug Discovery meeting

27thand 28th March 2022, Churchill College, Cambridge

Registration is now open


Synopsis:  The aim of the meeting is to continue the focus on case studies in Fragment-based Drug Discovery that have delivered compounds to late-stage medicinal chemistry, preclinical or clinical programmes. Over three-quarters of the presentations will be focused on case studies.




For over 30 years, the world’s leading life sciences companies have made Symeres part of their team. From hit generation and lead optimization, ADME-Tox via our Admescope organization, through to complex route development and clinical supply, we help to create safe, innovative therapies. We make molecules matter. Together.

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November 30, 2021
9th EFMC-YSN MedChemBioOnline 

May 8-11, 2022
Oegstgeest, The Netherlands
16th EFMC Short Course on Medicinal Chemistry New Opportunities in GPCR Drug Discovery

September 4-8, 2022
Nice, France
XXVll EFMC International Symposium on Medicinal Chemistry 

September 8-9, 2022
Nice, France
9th EFMC Young Medicinal Chemists' Symposium 


November 19, 2021
Liège, Belgium
MedChem 2021

January 24-28, 2022
3rd Alpine Winter Conference on Medicinal and Synthetic Chemistry

February 16-18, 2022
Rome, Italy
3rd Molecules Medicinal Chemistry Symposium (MMCS): Shaping Medicinal Chemistry for the New Decade

May 16-19, 2022
Volgograd, Russia
5th Russian Conference on Medicinal Chemistry


Senior Principal Scientist – Project Team Lead (80-100%*), Novartis Institute for BioMedical Research, Basel, Global Discovery Chemistry, Basel SWITZERLAND
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Medicinal Chemist, SpiroChem AG, Chemistry, Basel SWITZERLAND
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Research Scientist II in Radiochemistry, NOVARTIS, NIBR/GDC, Basel, SWITZERLAND
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Post Doc at Pharmacoinformatics Research Group, University of Vienna, Department of Pharmaceutical Sciences - Pharmacoinformatics Research Group, Vienna, AUSTRIA
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Drug Hunter @Aqemia, France (Paris) - deeptech startup leveraging AI and quantum-inspired physics for drug discovery, AQEMIA, Paris, Paris, FRANCE
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