IN MEMORIAM PAT WOSTER
It was with great sadness that we learnt of the death of Dr Patrick M. Woster, member of the MEDI Division of the American Chemical Society and former committee member of the series of joint events EFMC|ACSMEDI Medicinal Chemistry Frontiers. He greatly contributed to paving the way for a successful meeting series, and to building and maintaining the bridges between the European and American MedChemBio communities.
Dr Woster passed away July 15, 2023 after a courageous battle with cancer. The EFMC joins with all those who knew him in sending its condolences to his family, colleagues, friends and relatives.
A native of Omaha, Nebraska, Woster received a bachelor of science in pharmacy in 1978 and a Ph.D. in medicinal chemistry in 1987, both from the University of Nebraska Medical Center. He was a postdoctoral associate in chemistry at Rensselaer Polytechnic Institute and in medicinal chemistry at the University of Michigan.
He joined the Eugene Applebaum College of Pharmacy and Health Sciences at Wayne State University in 1988, rising to the rank of full Professor of pharmaceutical sciences by 2001. He joined MUSC in 2011, where he was appointed professor and SmartState® Endowed Chair in Drug Discovery and then department chair in 2015.
His research touched many areas, including the discovery of inhibitors of the polyamine pathway, novel antimalarial, antitrypanosomal and antibacterial agents, a variety of antitumor compounds, chemopreventive agents and epigenetic modulators. He is perhaps best known for the 1996 discovery (in collaboration with David Edwards) of 6,7-dihydroxybergamottin, the constituent in grapefruit juice that inhibits cytochrome P450 in the gut, altering the bioavailability of numerous therapeutic agents.
More recently, his research team published on the development of novel compounds that show early promise at fighting the rare pediatric cancer neuroblastoma when paired with the existing anti-cancer drug bortezomib (Velcade, Takeda Oncology). The novel compounds block or inhibit the lysine-specific demethylase 1 (LSD1).
Pat Woster memories
Pat Woster obituary
EFMC-ASMC 2023 – STILL POSSIBLE TO REGISTER!
Do not miss the opportunity to join the 500+ participants already registered for the IX EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry (EFMC-ASMC 2023), scheduled to take place in Zagreb, Croatia on September 3-7, 2023.
The programme will take place over 5 days, and will cover the most recent advances in new synthetic methodologies, total synthesis, chemical biology, process and medicinal chemistry, and automation & AI approaches in synthesis and drug discovery.
High level presentations include 27 invited lectures selected from both industry and academia, the EFMC Prize for a Young Medicinal Chemist or Chemical Biologist in Academia and in Industry lecture, as well as 9 oral communications.
More information and registration www.efmc-asmc.org.
We look forward to meeting you in Zagreb!
This contribution will focus on the recently published article on “Functionalized Cyclopentenones with Low Electrophilic Character as Anticancer Agents” by Késsia H. S. Andrade et al. focusing on the synthesis and first biological evaluation of functionalized cyclopentenones with low electrophilic characters and their potential in the development of anti-cancer drugs.
Cyclic enones have been known as potent cytotoxic agents however those compounds have toxic-related issues due to reaction with several critical biomacromolecules in vivo, likely caused by Michael addition to the enone system. Therefore the authors focused on the development of non-Michael acceptor cyclopentenones (CP) from furfural, a cheap furan derivative obtained from non-edible carbohydrate such as xylose.
Previous studies of the group illustrated that 2,4 substituted CPs were less prone to Michael addition making it a great starting point to develop their three derivatives: MCP (2-morpholino-4-thio-cyclopentenone), HCP (2-hydroxy-4-thio-cyclopentenone) and ACP (amino-4-thio-cyclopent-2-enones). Furfural was used to prepare 43 compounds via a tandem furan ring-opening/Nazarov electrocyclization and further functionalization.
The subsequent 2,4-substituted CPs exhibited were unreactive towards sulphur nucleophiles while maintaining cytotoxicity against HT-29, MCF-7, NCI-H460, HCT-116 and MDA-MB 231 cells lines. Unlike the commonly used enone cytotoxic agents, the new cyclopentenones lack the strong electrophilic character that leads to noxious side effects via unselective alkylation of critical macro biomolecules. Compounds showed promising IC50s as anticancer agents on certain cell line (below 10 mM) while being non-toxic against HEK-293 cells(at 20 mM). Additionally, while DCP (the initial trans-4,5-diamino-cyclopent-2-enone) and MCP lose their activity in estrogen receptor-negative breast cancer cells, the HCP family exhibits more activity in these cell lines. Furthermore, calculation of preliminary drugability parameters indicate drug-like properties following Lipinski’s rules of 5 and Veber’s rules.
Want to know more? Do not hesitate to take a look at the full story: https://doi.org/10.1002/cmdc.202300104
EFMC PHOTO CONTEST 2023 – BROWSE THE GALLERY!
"Illuminating Reality" is the topic of our 2023 Photo competition. We invited medicinal chemists and chemical biologists around the globe to submit a picture showing how their work contributes to “illuminating reality”.
The contest is now closed but voting is open!
Go and pick your favourite picture now! The 10 best shots will be selected to compete for the second round at the EFMC-ASMC 2023, where the prize winner and two runners-up will be announced!
Please enter your vote no later than August 15!
GET TO KNOW SOUFYAN JERHAOUI (JANSSEN PHARMACEUTICA NV, BELGIUM)
In this edition, our MedChemBioConversations is with Soufyan Jerhaoui from Janssen Pharmaceutica, Belgium. Get to know him better by reading the interview below:
How did you get interested in Medicinal Chemistry?
When I was studying chemistry, I had the exciting opportunity to perform a gap-year in industry which turnout out to be at Janssen. At the time I was working on Alzheimer’s disease and the potential impact of my work in addition to the company values increased my interest in medicinal chemistry.
I obtained my PhD at the University of Strasbourg under the supervision of Prof. Françoise Colobert, Dr. Jean-Pierre Djukic and Dr. Joanna Wencel-Delord. I graduated in October 2018. I was lucky to work on the hot topic of C-H activation, trying to use sulfoxides as chiral directing groups. Not only was I working on catalysis, but also total synthesis.
Where are you currently working and what is your current position?
I am currently working in Beerse, Belgium, as a Senior Scientist and team leader in the Discovery Chemistry department.
What do you like best about your work?
I’m constantly driven by trying to make a world without disease. My work has the potential to impact patients and it drives me every day to do my best. Besides, medicinal chemistry is a collaborative field, and every day is full of interaction and learning from my colleagues in different functions.
Which of your papers are you most proud of and why?
I enjoy collaboration in my work, and the papers I’m the proudest of usually result from collaborations. One example from my first year as a PhD student, I had the chance to give a talk at the JCO, an important conference held near Paris and gathering organic chemists from all around the world. After the talk, a research group engaged a conversation with me on the possibility to use our chiral auxiliary for their projects. Couple of years after, this nice collaboration gave a paper on sulfoxide-controlled aza-Piancatelli rearrangement.
What are the features of a successful PhD student or postdoc?
Curiosity and a collaborative mindset are two qualities that can help, not only during the PhD studies but during the whole career as a scientist.
What is the most embarrassing thing you have done in the lab while doing experiments, e.g. explosions?
Barely arrived at Janssen for a student internship, I started working on a challenging synthesis. After a few steps I realized that what I thought to be an impurity was in fact due to a two-carbon elongated starting material! Despite this misfortune, I learnt from my mistakes and since then I double check every product I use.
What are your recommendations for a book, podcast, website, blog, YouTube channel or film?
One of my colleagues, Matthew Horwitz, is leading Synthesis Workshop (https://synthesis-workshop.com/). I highly recommend looking at this website which highlights named reactions, total synthesis but also the human side of chemistry.
Which scientist do you admire the most and why?
That’s a tough question, as there are so many scientists who I admire even in my current work environment. But I would say Gertrude Elion. With Hitchings and Black, they brought the use of innovative methods for rational drug design. She also contributed to the development of drugs against leukemia, gout and malaria.
Which field of medicinal chemistry do you consider the most promising for the future?
I think that Artificial Intelligence and Machine Learning are and will be playing a critical role in our work, and it will certainly be interesting to see how medicinal chemists adapt to this emerging field. AI/ML can create a new revolution to be more efficient, and maybe help to advance emerging modalities like PROTACS.
EFMC SPONSORED EVENT REPORT: FRONTIERS IN MEDICINAL CHEMISTRY (FIMC) 2023
The Frontiers in Medicinal Chemistry (FiMC) 2023 symposium took place at the Lecture Hall Centre of the University of Vienna, Austria, from April 3-5 2023. At this international conference, recent advancements, innovative methodologies, and state-of-the-art technologies in Medicinal Chemistry were highlighted and recent Medicinal Chemistry case studies were presented. The meeting provided a vibrant platform for discussion among Medicinal Chemists from industry and academia. Moreover, outstanding contributions to Medicinal Chemistry were recognized and honored with the Friedrich Stolz-Award and the Innovation Award, jointly awarded by the Medicinal Chemistry Divisions of the German Chemical Society (GDCh) and the German Pharmaceutical Society (DPhG).
After two years of online events due to the COVID-19 pandemic, the Frontiers in Medicinal Chemistry (FiMC) 2023 conference took place as a face-to-face meeting again in the beautiful city of Vienna, Austria. Supported by the EFMC, the conference was organized by the Medicinal Chemistry Divisions of the German Chemical Society (GDCh) and the German Pharmaceutical Society (DPhG), together with the Division of Medicinal Chemistry of the Austrian Chemical Society (GÖCh), the Austrian Pharmaceutical Society (ÖPhG), and a local organization committee from the University of Vienna headed by Prof. Thierry Langer. The appealing program included 38 lectures by leading scientists from industry and academia as well as early career investigators. Overall, 102 posters were presented in two highly interactive poster sessions and the meeting gathered a total of 260 participants from 21 countries.
The conference started with the Medicinal Chemistry Highlights and Fresh Case Studies session, where recent work on KRASG12C and mutant KIT inhibitorsand TASK channel blockers was presented. In the following PhD Prize Award Ceremony Dr. Alaa Alhayek (Hirsch group, HIPS) and Dr. Li Gao (Thorn-Seshold group, LMU Munich) were awarded for their excellent work on pathoblockers and photoswitchable drugs, respectively. The day was rounded off with a session on New Chemistry and Modern MedChem Methods, a poster session and an informal get together. Highlights of the second day included a plenary lecture by Prof. Dirk Trauner on Adventures in Neuropharmacology, the Next Generation Drugs session organized by the NextGenMedChem group, and the prize ceremony for the Innovation Award, which was awarded to Dr. Matthias Schiedel in recognition of his pioneering work on intercellular GPCR ligands, fluorescent probes and PROTACs. Moreover, sessions like the Molecular Glues & Degraders and In Silico Solutions in MedChem as well as the Young Investigators featured a variety of excellent speakers. The second day of the meeting ended with another poster session followed by a great conference dinner. On the last day, the Translational Science Case Studies and RNA Modifying Enzymes sessions were succeeded by the Friedrich Stolz-Award ceremony, where Prof. Rolf Hartmann was honored for his outstanding achievements, especially in the field of steroid hormone biosynthesis inhibitors. After the two final sessions on Medicinal Chemistry Case Studies, three days of outstanding science ended with some closing remarks and the announcement of the poster price winners (Max E. Huber - University of Erlangen-Nürnberg; Lukas Schneider - University of Zürich; Tonia Kirschner - Technical University of Dortmund; Josef Braun- Technical University of Munich) and the NexGenMedChem best lecture award, which was given to Michael Hahn from Bayer for his presentation on TASK1/3 inhibitors.
The Frontiers in Medicinal Chemistry 2024 conference will take place from March 17-20th in Munich, Germany.
SUMMER SCHOOL ON PHARMACEUTICAL ANALYSIS 2023 (SSPA2023)
The SSPA is an international School which is addressed to PhD students, young researchers, and professionals from private companies. The 2023 edition will focus on “Analytical methods for drug manufacturing and quality control” and will take place on September 11-13, 2023 in Rimini, Italy.
- Pharmacopeias, Guidelines, GMP regulation et al.
- Structural Analytical Chemistry: NMR, spectroscopy
- Analytical aspects related to API development and manufacturing
- Analytical aspects related to Drug Product development and manufacturing
- In Process Control & Cleaning Verification
- Analytical Method Development and Phase-Appropriate Method Validation
- Analytical Aspects for Inhalation products
- Physical Properties and Solid State Characterization
- Stability Studies
- Microbiology Testing and Environmental monitoring
- Case studies: eparine and nitrosamine
Lectures will be delivered by recognised experts from the industrial and academic sectors. The school social activities are planned to promote networking and favor interactivity between participants and lecturers. To maximize these aspects the number of in-person participants is limited to 80, however, the school is also offered as hybrid event.
More information and registrations on https://www.sspaweb.com/index.asp.
Contact: Marina Rinaldi (firstname.lastname@example.org)
A JOB or PHD/POST-DOC POSITION TO SHARE? USE OUR JOB PORTAL
The posting of Job/PhD & Post-Doc open positions is free and is available for any MedChemBio related job, for example, industry and academic positions.
Job posting is now made even simpler, you only have to provide the URL of the job application.
Once reviewed, the position will be available on the EFMC website and in the monthly newsletter "MedChemBioWatch".
NEWS FROM THE BIOLOGICAL AND MEDICINAL CHEMISTRY SECTOR (BMCS) OF THE ROYAL SOCIETY OF CHEMISTRY (RSC)
The BMCS is pleased to announce its upcoming events.
- SCI/RSC 22nd Medicinal Chemistry Symposium
- 6th RSC-BMCS/RSC-CICAG Artificial Intelligence in Chemistry
- Hot Topics: Targeting RNA
- RSC-BMCS Postgraduate symposium XVII
- 9th RSC-BMCS Fragment-based Drug Discovery Meeting
- The BMCS Mastering MedChem VIII: 8th RSC-BMCS Symposium on Mastering Medicinal Chemistry
- 35th Medicinal Chemistry in Eastern England (Hatfield symposium)
- 3rd RSC / SCI / SEQT New Therapeutics for Global Health
SCI/RSC 22nd Medicinal Chemistry Symposium
10th – 13th September, 2023, Churchill College, Cambridge, UK
Registration is open!
Synopsis: The organisers invite you to the 22nd SCI-RSC Medicinal Chemistry symposium, Europe’s premier biennial Medicinal Chemistry event, focusing on first disclosures and new strategies in Medicinal Chemistry
6th RSC-BMCS/RSC-CICAG Artificial Intelligence in Chemistry
4th – 5th September, 2023, Churchill College, Cambridge, UK
RSC BMCS/RSC CICAG
Registration is now open!
Synopsis: Artificial Intelligence is experiencing a renaissance in the development of new methods and practical applications to ongoing challenges in Chemistry. Following the successes of five annual “Artificial Intelligence in Chemistry” meetings starting in 2018, we are pleased to announce that the Biological & Medicinal Chemistry Sector (BMCS) and Chemical Information & Computer Applications Group (CICAG) of the Royal Society of Chemistry are once again organising a conference to present the current advances in AI and machine learning in Chemistry. The meeting will be held over two days and combine aspects of artificial intelligence and deep machine learning methods to applications in chemistry. The programme will include a mixture of keynote talks, panel discussion, oral presentations, flash presentations, posters and opportunities for open debate, networking and discussion.
Hot Topics: Targeting RNA
30th November 2023, Virtual
Registration is now open!
Synopsis: The BMCS Hot Topics online meetings are intended to highlight breaking areas of research in fields of science relevant to drug discovery. They will run as stand-alone half-day virtual events, 2-3 times per year. The programme will be targeted towards researchers working in academia or industry who would like to enhance their understanding of these nascent or developing fields. The inaugural meeting will cover relevant methods and modes of targeting RNA in drug discovery and will focus on how small molecules can accomplish this, including RNA binding and degradation, splicing modulation, and enzymes modifying RNA. There will be presentations from leading academics and industry.
RSC-BMCS Postgraduate symposium XVII
7th December 2023, University of Oxford, Oxford, UK
Abstract submissions are now open!
Registrations are now open!
Synopsis: This face-to-face meeting will comprise an oral and poster presentations from PhD students and post-doctoral workers researching in biological or medicinal chemistry. In addition, the agenda will feature invited keynote speakers from industry and academia.
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EFMC ORGANISED EVENTS
September 3-7, 2023
IX International Symposium on Advances in Synthetic and Medicinal Chemistry (EFMC-ASMC)
September 7-8, 2023
10th EFMC Young Medicinal Chemists' Symposium (EFMC-YMCS)
September 26, 2023
16th EFMC-YSN MedChemBioOnline
November 16-18, 2023
EFMC International Symposium on Chemical Biology (EFMC-ISCB)
EFMC SPONSORED EVENTS
September 17-20, 2023
National Meeting on Medicinal Chemistry (NMMC28)
September 20-22, 2023
Vila Real, Portugal
I International Meeting Molecules4Life
September 26, 2023
3rd Munich-Leiden Virtual ChemBio Talks
October 10-11, 2023
MedChem Campus 2023
December 7, 2023
Oxford, United Kingdom
RSC-BMCS Postgraduate Symposium XVII
December 8, 2023
January 24-26, 2024
SCF Chemical Biology Symposium 2024 – Chemistry meets Biology
January 28-February 1, 2024
St. Anton, Austria
4th Alpine Winter Conference on Medicinal and Synthetic Chemistry
September 10-15, 2023
Vienna Summer School Drug Design
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