EFMC STATEMENT ON THE INVASION OF UKRAINE
EFMC strongly condemns Russia's invasion of Ukraine and expresses its support to the scientific community and to the Ukrainian people. Your courage and resilience are to be praised, and our thoughts are with you.
We urge the leaders at national, European, and international levels to work towards a quick and peaceful end to this situation.
PROMOTING GENDER DIVERSITY IN THE EFMC AWARDS & PRIZES
It was with pleasure that the EFMC received this year again many high-quality nominations for our various Awards & Prizes. We are always honoured to see so many worthy candidates being suggested!
For some awards, and especially those recognising life-long career achievements, we are noticing a lack of gender diversity in the nominees. While it is appreciated by all that consideration for diversity was less preeminent in the past and that the scientific heroes who helped shaping a better world must be fully recognised, it is the duty of the community to also showcase the pioneering figures that might remain shadowed otherwise.
As usual, our various international committee will promote the EFMC values of scientific excellence, honesty, fairness, and diversity in making their unbiased selection – but it is the mission of the whole community to help them in the future in putting forward those worthy candidates who showcase the diversity of our field.
On behalf of EFMC, I want to personally thank all applicants and nominators...and may the best candidate win!
The “literature spotlight” section of the newsletter will bring you a summary of 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 EFMC working groups.
This contribution will focus on the recently published article on “Design and Synthesis of Highly Selective Brain Penetrant p38α Mitogen-Activated Protein Kinase Inhibitors” by Tormählen, N. M., Martorelli, M., Kuhn, A., Maier, F., Guezguez, J., Burnet, M., ... & Koch, P. (2021) - Journal of Medicinal Chemistry.
Neurodegenerative diseases are a challenging area for the medicinal chemist; in this week’s literature spotlight, we choose to focus our attention on the research of Tormählen, from Tübingen University in Germany.
Neuroinflammation and neurodegeneration are phenomenon linked to cytokine overproduction that can be induced by p38α mitogen activated protein kinase (MAP kinase). However, developing aprotein kinase inhibitor against neurodegenerative disease can be quite challenging when selectivity, blood brain barrier permeation and metabolic stability have to be balanced.
This study focuses on the development of new inhibitors of p38α MAP kinase derivated from previous study of the group that discovered the potency of Skepinone L and Skepinone N on this peculiar target. From these first derivatives, SAR were explored and two hydrophobic regions were discovered allowing the authors to attain a deeper understanding of the target. The main objective of this study was to build a library of compounds with potent selective activity, metabolic stability, and capacity to cross the blood brain barrier (BBB).
In the first part of the paper, the authors described the synthesis of 62 novels Skepinone based p38α MAP kinase inhibitors with nanomolar range activity regardless of the C3 substituent (lipophilic, basic, amino acid derivative, etc.). The main strategy adopted to enhance absorption was the use of an ester prodrug, which would be able to cross the BBB. Other strategies were investigated such as the modifications to the pendant amino acids to promote the BBB permeation with amino acid transporters.
After confirming the potency of their analogues, the authors checked the metabolic stability of 21 of their best compounds proving the stability of the carboxylic acid and the metabolic instability of the ester derivative in human liver microsomes (HLM). A second step of analysis was performed on 15 of those compound to assess their brain permeation and plasma stability in male RjOrl:Swiss CD-1 Mice. Most confirmed the preliminary data obtained in the HLM assay. To study the anti-inflammatory property of those compounds, further in vitro and in vivo studies were performed on twelve derivatives. Splenocytes and Balb/c mouse whole blood were stimulated to promote cytokines, IL-6 and TNFα production; all the compounds appeared to decrease that production in a dose dependent manner. Cytotoxicity was also assessed at this stage. The transgenic mouse C57BL/6 was used as a neurodegenerative model for determining the pharmacokinetic and BBB permeation for seven derivatives, showing a better BBB permeation for Skepinone-N derivatives. Finally, after hERG and CYP inhibition evaluation, a selectivity assay against a kinome was performed in order to select the most promising compound.
This study demonstrated the complexity of medicinal chemistry required in neurodegenerative disease drug discovery. From a library of 62 compounds, only one had all the desired properties to be selected as a hit compound. The compound 70 (derivated from Skepinone N) was thus selected as a promising lead compound thanks to its good selectivity, CYP, hERG interaction, and high partition into the CNS.
Read the article: https://pubs.acs.org/doi/10.1021/acs.jmedchem.0c01773
EFMC GRANTS – APPLICATIONS DEADLINE IS MARCH 15
EFMC is funding grants for EFMC organised events with the aim to support the participation of young academic scientists. Upon application, a limited number of grants will be covered by EFMC, corresponding to:
- Ten grants covering the full registration fees for the XXVII EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2022) and the 9th EFMC Young Medicinal Chemists' Symposium (EFMC-YMCS 2022).
To apply for an EFMC grant, please fill in the application form and upload your CV, publication list, abstract, motivation letter, and support letter from the supervisor.
More information, deadlines, and application on www.efmc.info/ysn-grants
EFMC SUPPORTS THE “STICK TO SCIENCE INITIATIVE”
EFMC is proud to support the ‘Stick to Science’ campaign, launched on 8 February, urging EU leaders, as well as the UK and Swiss governments, to place science collaboration before politics, and to quickly reach the UK’s and Switzerland’s association to Horizon Europe. Since the launch, the campaign has reached close to 4 million people on Twitter, and gathered a total of over 3400 signatures.
If you have not signed up to the initiative yet then please do so! These signatures are important in ensuring that we get the attention of European leaders and secure association to Horizon Europe. The initiative is open for all to sign, both as an individual or as an organisation on the dedicated website.
The site also includes a range of resources for supporters, including suggested social media posts, banners, and email signature templates.
EFMC-ISMC 2022 – DEADLINE FOR OC SUBMISSION AND EARLY BIRD FEE IS MARCH 24!
The XXVll EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2022) is organised by the Société de Chimie Thérapeutique (SCT), on behalf of the European Federation for Medicinal Chemistry and Chemical Biology (EFMC).
The event will take place in Nice, France on September 4-8, 2022. The organisers are confidently planning for a in-person live event, with hybrid options if the situation requires it. Access to the conference will be limited to fully vaccinated individuals.
Calendar of Abstract Submissions
- Deadline for Oral Communication submission and free Poster submission: March 24, 2022
- Announcement of accepted oral communications: mid-May, 2022
After March 24, 2022 and until June 23, 2022, abstracts for Posters can still be submitted, but with a handling fee of 50,00€
GET TO KNOW DENNIS GILLINGHAM (UNIVERSITY OF BASEL, SWITZERLAND)
In this edition, our #Iamamedicinalchemist is Prof. Dennis Gillingham (University of Basel, Switzerland).
Get to know him better by reading the interview below:
How did you get interested in Medicinal Chemistry?
Through natural product total synthesis; I was always impressed by what Nature’s bounty could achieve in modulating biology and wanted to try my hand at it.
Where and when did you obtain your PhD diploma?
Boston College, 2007
What was the topic of your PhD project
Total synthesis of a marine natural product of no known use
Where did you have your postdoc position?
ETH Zürich, with Prof. Donald Hilvert
Where are you currently working and what is your current position?
Associate Professor of Chemistry, University of Basel
What are your current research interests?
Performing complex chemistry on DNA as well as using small molecules to degrade proteins
How would you explain what your research area is to non-scientists?
Designing precision tools on the molecular scale to change biological processes
What do you like best about your work?
Always new problems to solve, always new stuff to learn
What kind of tasks does your work involve?
Considering problems in biology and designing molecules to study those problems
What kind of skills does your work require?
Synthetic chemistry, cell biology, molecular biology, analytical chemistry
What do you consider your greatest achievement in your scientific career?
I can’t point to one discovery. Looking back over an area of research with many discoveries is what I consider achievement.
Which of your papers are you most proud of and why?
This paper outlines our discovery that suitably placed boronic acids accelerate and improve oxime formations. We studied it as a bioconjugation tool and it continues to be used in many areas.
An unusual and unexpected discovery for us: copper carbenes, which we thought would be extremely reactive, can actually deliver clean synthetically useful modifications of nucleic acids.
We executed a large complex synthesis on DNA, pushing the synthetic limits of on-DNA chemistry.
How many PhD students and postdocs do you currently supervise?
Are you currently looking for a new PhD student or a postdoc?
Currently we are 13 people and could expand to 15.
What are the features of a successful PhD student or postdoc?
Fearlessness: The willingness to step outside of your comfort zone and learn new things.
How would you describe yourself as a supervisor?
Curious, attentive, willing to help.
What is the most embarrassing thing you have done in the lab while doing experiments, e.g. explosions?
Refluxing reaction exploded, stunk out the whole building…leading to an “investigation”.
What are your recommendations for a book, podcast, website, blog, YouTube channel or film?
Anything by Steven Pinker, Richard Dawkins, Hans Rosling
Which scientist do you admire the most and why?
Steven Pinker – For his ability to change the world with simple logic and accessible argumentation.
Have you experienced any unfair situations during your scientific career?
Absolutely, but many people of different skin colour or gender than me have had it much worse.
Which field of medicinal chemistry do you consider the most promising for the future?
Building molecules that are capable of executing complex functions.
What advice would you give to someone who wants to know more about your field?
Come and work in my lab.
What would you like to ask from other medicinal chemists?
Send your best students to my lab.
What would you expect to be the next major breakthrough in medicinal chemistry?
Small molecules collaborating with biologics in immunoncology
BEST PRACTICES IN MEDICINAL CHEMISTRY EPISODES 1-3 AVAILABLE!
Have you ever wondered how medicinal chemists work in other companies or in academia? Are there important trends or new technologies that you may have missed? In these rapidly evolving fields, there are only few opportunities to share best practices among industry and academic practitioners.
We can of course learn from case studies presented at conferences, but wouldn’t it be great to also have material covering more general concepts? Following the initiative of Jean Quancard, the EFMC assembled a team of experienced practitioners from industry and academia to deliver freely accessible webinars and educational slide decks for distribution and teaching.
- Episode I - Validating Chemical Probes
- Episode II - Phenotypic Drug Discovery (PDD)
- Eoisode III - Hit Generation
High quality chemical probes are essential to explore human biology and diseases and, as chemists, we have a big role to play to ensure high quality of the published probes.
Phenotypic drug discovery (PDD) has contributed to the discovery of many innovative drugs and has received growing attention over the last few years. Learn about the opportunities and challenges of phenotypic drug discovery and share best practices utilised in industry and academia.
Hit generation is a crucial step in the drug discovery process. Accessing high quality hits will greatly increase the speed and chance of success to identify drug candidates. Discover current approaches to generate and validate hits, and the importance of having an integrated strategy combining several approaches
Want more? Stay tuned as the team will be releasing the fourth episode “Tactics: how to select the right starting points” in the upcoming months!
THE MEDICINAL CHEMISTRY DIVISION OF THE ITALIAN CHEMICAL SOCIETY AND CHEMICAL BIOLOGY
Since its establishment as a learned society, the Italian national society member of the EFMC (Divisione di Chimica Farmaceutica - Società Chimica Italiana; Medicinal Chemistry Division of the Italian Chemical Society, DCF-SCI) included medicinal chemists from academia and industry interested in the discovery and development of new therapeutic agents as well as in the design and use of molecules as tools to probe biological systems, from protein structure and function, to cellular pathways, to complex organisms.
Therefore, the decision to integrate “chemical biology” in the name of EFMC aligned perfectly with the mission of DCF-SCI. Like other National Adhering Organizations, DCF-SCI considers both disciplines as part of a continuum. The only reason why it did not adapt its name to include chemical biology visibly was to avoid confusion with another Division of the Italian Chemical Society dealing with biological chemistry.
In fact, chemical biology has long been included in DCF-SCI's events. For instance, the Italian national symposium NMMC (the 27th edition will be held in Bari, September 11–14 2022) always include chemical biology topics. Similarly, the 2022 edition of the European School of Medicinal Chemistry (ESMEC, Urbino, July 3–7 2022) will cover new modalities for targeting challenging proteins and the Summer School on Pharmaceutical Analysis (SSPA, Rimini, September 21–23 2022) will be focused on bioanalytical methods.
For additional thoughts regarding the chemical biology–medicinal chemistry continuum, please see ChemBioChem, 2021, 22, 2823. Additionally, the first of the series of webinars and slide decks of the EFMC Best Practice Initiative is dedicated to the generation and validation of high-quality chemical probes, which are critical for drug discovery and more broadly to further our understanding of human biology and disease (ChemMedChem 2020, 15, 2388).
REPORT – 3rd ALPINE WINTER CONFERENCE ON MEDICINAL AND SYNTHETIC CHEMISTRY
Aiming to continue the mission to expose attending scientists to cutting edge synthetic and medicinal chemistry as well as latest developments in technologies that foster innovation in drug discovery, the 3rd edition of the Alpine Winter Conference on Medicinal and Synthetic Chemistry ran as a fully virtual event on January 24-28, 2022.
Organised by the International Forum for Biomedical Research (IFBR) and hosted by Dr Klemens Hoegenauer (Novartis, CH), Dr Karl Heinz Krawinkler (Novartis, CH) and Dr Antonia Stepan (F. Hoffmann-La Roche, CH), the event gathered 173 attendees behind their screens for a week of half-day sessions.
The participants attended a high-quality programme (average rating 4.1 on a scale from 0-5) of three keynote lectures and eight themed sessions gathering 26 invited lectures and 6 oral communications from submitted abstracts. Highlights of the programme included the keynote lectures by Prof Angela Koehler (MIT, United States), Prof. Paul Knochel (Ludwig Maximilians University, Germany) and Dr Wendy Young (MPM Capital, United States).
The individual sessions of the conference:
- Automation and Machine Learning Applications for Medicinal Chemistry
- Covalent Targeting: Innovating for the Future
- Drug Discovery Tales
- Increasing sp3 Fragment Options: Advances in the Synthesis of Small Ring Systems
- Methodologies to Understand Cellular Target Interaction
- Targeting Unstructured Proteins
- The "Catalytic Cycle" of Complex Molecule Synthesis and Methodology Development
- Understanding PK and PK/PD relationships in drug discovery - Target Mediated Drug Disposition
Despite the virtual format, the organisers offered many networking opportunities to connect individual participants with each other. The virtual conference centre offered a chat system, video calls, interactive poster sessions, and virtual exhibitions.
The Scientific Organizing Committee thanks all attendees for their active participation at the virtual edition of the Alpine Winter Conference and is looking forward to welcoming you all to St. Anton, Austria in January 2024!
NEWS FROM THE FRENCH MEDICINAL CHEMISTRY SOCIETY (SCT)
Evotec, in partnership with the French Medicinal Chemistry Society, is delighted to invite submissions for a new “Prize for Excellence in Molecular Design” to be awarded to an exceptional young to mid-career scientific research talent from academia or industry.
The successful candidate will be selected based on outstanding innovation and applied state-of-the-art molecular design skills that have contributed to a demonstrated advance to drug discovery boundaries. In particular, the assessment panel are keen to recognise “molecular architects” that have demonstrated excellence in drug design via a rational approach to the data analysis and design phase resulting in highly informative novel molecules or drug candidates that have significantly advanced a drug discovery project.
Submissions should be the subject of a published (or accepted) scientific article preferably, to cover a “breakthrough” discovery or innovative technology, and may include the application of machine-learning and/or artificial intelligence (AI).
• The amount to be awarded is three thousand euros (3 000 €).
• 31st March 2022 (at midnight)
• The successful candidate will be a “molecular architect” who has demonstrated adventurous and creative qualities to push the boundaries of the industry’s current thinking in drug design and data analysis.
• The candidate should clearly demonstrate that they has significantly contributed to aspects relevant to excellence in molecular design within discovery research projects.
• The candidate must have published a key article illustrating innovation in molecular design or should be able to demonstrate that such publication is likely to be accepted.
• The candidate should be an “early to mid-career researcher” and have a valid membership to the EFMC throughout their national EFMC-adhering organisation (NAO).
Award Holder obligation
On top of the mandatory affiliation to one of the European Federation for Medicinal Chemistry and Chemical Biology (EFMC) adhering societies for the year of application, the Award Holder should respect ethical criteria:
1. To promote SCT and EFMC among his network, and to be an EFMC-adhering society member at least one additional year after receiving his prize.
2. To promote the sponsor along his network, according to some pre-rules established with them.
3. To give a lecture at one of the SCT scientific events decided between SCT and EVOTEC.
• The candidacy report (5 pages maximum) should present a full description of the innovation, including the state-of-art-design, the context and the exceptional added value of the innovation plus potential downstream value, plus any references/publications/patents, and a short CV of the candidate.
• This should be sent in a single pdf file named: EVOTECPrize_NAME_FirstName.pdf to secretary(at)sct-asso.fr and president(at)sct-asso.fr before the stated deadline.
NEWS FROM THE DIVISION OF MEDICINAL CHEMISTRY OF THE GERMAN CHEMICAL SOCIETY (GDCH)
The German Chemical Society (GDCh) and the German Pharmaceutical Society (DPhG) cordially invite you to attend the annual meeting on "Frontiers in Medicinal Chemistry" which will be held online on March 13 -16, 2022.
The international symposium will focus on current developments, novel approaches and cutting-edge technologies in the field of medicinal chemistry and drug research with sessions on: Non-Mainstream Chemotypes, Chemical Epigenetics, First Disclosures & Case Studies, Next Generation Drugs, Macrocycles, AI–Retrosynthesis and Automation, Medicinal Chemistry and Target Highlights, Young Investigators.
The scientific program will include lectures, and poster presentations. It is the goal of the organisers to make this meeting an event of scientific excellence, attractive to both industrial and academic scientists in Medicinal Chemistry, Chemical Biology, and related fields of research.
More information and registration available here.
NEWS FROM THE BIOLOGICAL AND MEDICINAL CHEMISTRY SECTOR (BMCS) OF THE ROYAL SOCIETY OF CHEMISTRY (RSC)
The BMCS is pleased to announces some upcoming events:
- 8th RSC-BMCS Fragment-Based Drug Discovery Meeting
- 33rd Medicinal Chemistry in Eastern England (Hatfield Symposium)
- 2nd Synthesis in Drug Discovery and Development Meeting
Fragments VIII: 8th RSC-BMCS Fragment-based Drug Discovery meeting
27thand 28th March 2022, Churchill College, Cambridge
Delegate Registration and Exhibitor/Sponsor 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.
33rd Medicinal Chemistry in Eastern England (Hatfield symposium)
28th April 2022, The Fielder Centre, Hatfield, UK
Delegate Registration and Exhibitor/Sponsor registration is now open
Synopsis: Known colloquially as the "Hatfield MedChem" meeting, this a highly successful, long-standing, one-day meeting that runs annually. The scientific program will comprise of presentations showcasing medicinal chemistry case studies from tools to candidates, across a range of modalities, therapeutic areas, and target classes, as well as covering more general topics from the forefront of drug discovery of relevance to medicinal chemists.
2nd Synthesis in Drug Discovery and Development meeting
4thto 5th May 2022, virtual
Delegate Registration and Exhibitor/Sponsor registration is now open.
Synopsis: Synthesis is at the heart of drug discovery and development. The industry has increasingly demanded higher quality clinical candidates and has sought to exploit less druggable biological targets. Successful programmes require the application of innovative synthesis in all stages of discovery and development. The medicinal chemist’s toolbox is also enhanced by the introduction of novel bioisosteres, often made available only through the application of new synthetic methods. This symposium aims to celebrate the crucial role of synthesis in the success of drug discovery and development.
THIS NEWSLETTER IS KINDLY SPONSORED BY
ISSUE SPONSORED BY
Oxeltis seasoned medicinal chemist team provides hit and lead optimization services, and expertise in particular areas of multi-step organic synthesis: heterocycles, macrocycles, nucleosides/nucleotides, modified sugars and oligo/polysaccharides. The team focuses on speed, quality and confidentiality in the services and collaborative ventures that it develops.
EFMC ORGANISED EVENTS
May 8-11, 2022
Oegstgeest, The Netherlands
16th EFMC Short Course on Medicinal Chemistry New Opportunities in GPCR Drug Discovery
September 4-8, 2022
XXVll EFMC International Symposium on Medicinal Chemistry
September 8-9, 2022
9th EFMC Young Medicinal Chemists' Symposium
EFMC SPONSORED EVENTS
June 15-17, 2022
Chemical Sciences in Biological Challenges
June 19-22, 2022
Santiago de Compostela, Spain
XX National Meeting of the Spanish Society of Medicinal Chemistry
July 27-29, 2022
3rd Molecules Medicinal Chemistry Symposium (MMCS): Shaping Medicinal Chemistry for the New Decade
September 15-17, 2022
9th BBBB International Conference on Pharmaceutical Sciences - Pharma sciences of tomorrow
(Senior) Scientist Medicinal Chemistry, Proxygen GmbH, Chemistry Vienna, AUSTRIA
Team Leaders - Synthetic Organic and Medicinal Chemistry, BioAscent Discovery Ltd., Chemistry Newhouse, UNITED KINGDOM
Synthetic Organic and Medicinal Chemists - Scientists and Senior Scientists, BioAscent Discovery Ltd., Chemistry
Newhouse, UNITED KINGDOM
Team Leaders - Synthetic Organic and Medicinal Chemistry, BioAscent Discovery, Recruitment
Glasgow, UNITED KINGDOM
Resourcing Consultant, BioAscent Discovery, Recruitment
Glasgow, UNITED KINGDOM
Research Associate Medicinal Chemistry (PhD), Evotec, Medicinal Chemistry
Group Leader in Medicinal Chemistry, Evotec, Medicinal Chemistry
Medicinal Chemist, SpiroChem AG, Chemistry, Basel, SWITZERLAND