MedChemWatch
Monthly Newsletter January 2020

BEST WISHES FROM EFMC

At the beginning of our 50th anniversary year, we would like to wish you a very happy and successful 2020.

EFMC RECOGNITION PROGRAMME – EFMC HONORARY FELLOWS

To kick off our 50th anniversary celebrations, we would like to recognise the immense contribution of those who not only brought EFMC into being in 1969 but have helped to make it what it is today. We are, therefore, very proud to announce the award of the first EFMC Honorary Fellows. The first recipients have created and nurtured the mission and vision of EFMC during its first 50 years. All are former Presidents but have been contributors above and beyond and remain active supporters of EFMC. Congratulations and thanks to:

• Prof. Henk Timmerman (VU University, The Netherlands)
• Prof. Ferran Sanz (Universirty Pompeu Fabra, Spain)
• Prof. Roberto Pellicciari (TES Pharma, Italy)
• Prof. Gerhard Ecker (University of Vienna, Austria)
• Prof. Uli Stilz (Novo Nordisk, Denmark)
• Prof. Koen Augustyns (University of Antwerp, Belgium)

Additionally, due to his contribution in launching the series of EFMC-YMCS events, we are happy to recognize also:

• Prof. Chris De Graaf (Heptares Therapeutics, United Kingdom)

The official ceremony will take place during the opening of the XXVI EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC 2020), scheduled to take place in Basel, Switzerland from September 6-10, 2020.

The EFMC recognition programme will continue awarding outstanding contributors to EFMC and sciences in the future with a system of open call for nominations – to be launched in fall 2020.

THE EFMC YEARBOOK 2020 IS NOW AVAILABLE

The official EFMC Yearbook 2020, "Medicinal Chemistry in Europe" is a valuable resource for those interested in quickly finding information on all things EFMC, such as the activities and composition of Member Societies, Corporate Members and the activities and events of EFMC and its working groups. It is available to view online or to download and keep.

View online

Download the PDF

EFMC AWARDS & PRIZES: NOMINATION DEADLINE IS APPROACHING

To acknowledge outstanding achievements in the field of Medicinal Chemistry and Chemical Biology, EFMC will confer several awards & prizes in 2020.

The deadline for nominations is January 31 !

GET TO KNOW SOUVIK SARKAR (UMEA UNIVERSITY, SWEDEN)

The first #Iamamedicinalchemist of 2020 is Souvik Sarkar from Umea University, Sweden.

Want your story to be published!? Contact us at communication@efmc.info

 

How did you get interested in Medicinal Chemistry?
Since childhood, I wanted to be a scientist. During my masters in Chemistry, the concept of drug discovery used to fascinate me. So, I explored my passion and interest in the field of medicinal chemistry to develop new drug candidates against evolving disease conditions for the benefit of mankind.

Where and when did you obtain your PhD diploma?
I was awarded my PhD diploma from CSIR-Indian Institute of Chemical Biology, University of Calcutta in 2016

What was the topic of your PhD project?
My Ph.D. research focused on the design, synthesis and biological evaluation of phenolic molecules against inflammatory diseases and cancer. During my doctoral studies, I synthesized polyphenolic small molecules as the inhibitor of macrophage migration inhibitory factor (MIF) and studied their effect on cancer cell proliferation as a result of altered mitochondrial pathology, where MIF plays a significant role. I also examined the role of these polyphenolic compounds as antioxidants against NSAID-induced gastric mucosal injury by the amendment of mitochondrial oxidative stress. In another project, I have synthesized novel antimalarial hydrazone compounds having promising antimalarial activity against multidrug resistant strains.

Where do you work at the moment and what is your current position?
I am currently working as a Senior Research Engineer under the supervision of Prof. Fredrik Almqvist, Department of Chemistry, Umea University, Sweden.

What are your current research interests?
I am working on the design, synthesis and development of Mycobacterium Tolerance Inhibitors (MTIs) that invoke collateral sensitivity in Mycobacterium tuberculosis (Mtb). These MTIs sensitize Mtb to stresses during infection and restore activity to the frontline antibiotic isoniazid (INH) in otherwise INH-resistant katG mutant Mtb isolates.

What do you like most in your job?
As a medicinal chemist, I relish to encounter and troubleshoot unfamiliar challenges in the laboratory. I find it extremely satisfying when my tiring efforts in synthesis produce active compounds against the disease models, I am working with. Apart from the lab work, I also appreciate the versatility of my job that involves writing, exchanging ideas with the collaborators, presentations, seminars and so on.

What kind of skills your job requires?
My job requires the skill of handling delicate reagents and intermediates with highly reactive functional groups. The strong knowledge in multistep synthesis, pharmacophore designing, and biological studies are also obligatory to meet the responsibilities of my job.

What do you consider your biggest achievement in your scientific career?
I am highly privileged to actively work in a project with NIH-approved grant during my post-doctoral studies. This study shows the unique potential of our compound to reverse Isoniazid (INH) resistance. Our findings hold a promising avenue to disarm INH resistance in the clinic, offering contribution in combating the global epidemic of TB.

What are the features of a successful PhD student or postdoc?
A PhD student must be highly motivated, inquisitive and hardworking to pursue his/her scientific research. The responsibilities of a post-doctoral researcher include independent thinking to develop a project, dynamic networking, and inspire the PhD students to cultivate their insights to thrive to explore their scientific pursuits.

What is the most embarrassing thing you did in the lab while doing experiments?
Once I turned my chemical hood yellow along with the instruments and solvent bottles by an explosion during a nitration reaction.

Which scientist do you admire the most and why?
Prof. Phil Baran at Scripps Research Institute. He performs robust synthetic chemistry work which has implications in medicinal chemistry, agrochemicals and industries. In his lab they did chemical reactions in a cup of coffee or plastic bucket to show the synthetic procedures are easy and robust. He is changing the view of organic chemists by breaking the myth about the synthesis of complicated compounds with efficient simple transformations.

Which paper of yours you are the proudest of and why?
As I have mentioned earlier, I am proud to work in an NIH-funded project. One of our recent investigations was published in PNAS (Proc Natl Acad Sci U S A.) that depicted a novel avenue to reverse antibiotic resistance in persistent tuberculosis strains.

Which field of medicinal chemistry do you consider the most promising in the future?
In my opinion, personalized medicine is the most promising advancements in next-generation therapeutic intervention, especially in the treatment of cancers; because it will replace the “one size fits all” concept of therapies, where same dose of drugs is prescribed to all the patients. This kind of therapy is tailored to consider the genetic and biological makeup, the environment and lifestyle of each and every individual

What would you like to ask from other medicinal chemists?
I would be interested to perceive the rationale of other medicinal chemists in pharmacophore designing. I would also prefer to seek out their notion about target identification minimizing off-target effects.

What would you guess to be the next major breakthrough in medicinal chemistry?
I realized that acquired drug-resistance is the major challenge in medicinal chemistry. Development of novel drugs that can reverse the drug-resistance mechanism can be the cornerstone to fetch the revolution in therapeutics.

REPORT OF THE 13TH RSC-BMCS BIOLOGICAL AND MEDICINAL CHEMISTRY POSTGRADUATE SYMPOSIUM

The 13th BMCS Biological and Medicinal Chemistry Symposium, held in Cambridge on Friday 13th December 2019, was the latest in the annual series designed to showcase the very best postgraduate research in the fields of biological and medicinal chemistry.

It attracted an audience of over 160 registered attendees who heard three plenary lectures and 8 student lectures. There were also 19 poster presentations and the quality of the science presented was yet again extremely high. The symposium also included a Flash Poster session, where the poster presenters ‘pitch’ a 2-minute slide to the audience to attract them to their poster; a format which has always generated lots of discussion afterwards.

There were also three plenary speakers, all of whom highlighted the key influences in their career path as well as outlining some of the science they are involved in – Angela Russell (University of Oxford), Tilly Bingham (Concept Life Sciences) and Emma Carswell (Cancer Research UK - Therapeutic Discovery Laboratories).

The overall winner for the best oral communication was Jessica Reynolds from the University of Oxford (‘Design and Synthesis of Chemical Tools to Probe the Function of TRIM33’) while the runner-up was Gemma Davison from the Northern Institute of Cancer Research (‘FragLites: Minimal, Halogenated Fragments Displaying Pharmacophore Doublets, an Efficient Approach to Druggability Assessment and Hit Generation).

The prize for the best poster communication went to Josie Gaynord from the University of Cambridge (‘Stapled peptide-drug conjugates with antimicrobial activity’), who received a cheque for £250, while the runner up prize and the participant’s prize went to Emily Faulkner from the University of Leeds (‘The Design, Synthesis and Biological Evaluation of Nitrogen Containing Heterocyclic Fragments against Aurora A Kinase’) and Adam Thomas from the University of Oxford (‘A CRISPR Method For Rapid In-Cell Validation of Epigenetic Targets’), respectively.

Apart from receiving a cheque for £500, Jessica will also represent the UK at the Young Medicinal Chemists Symposium in Basel on 10th and 11th September 2020. All the prize awardees were given an RSC certificate commemorating their achievement and one year’s e-subscription to RSC Medicinal Chemistry. Ellen and the poster prize-winners will also be awarded bursaries to attend the ‘Mastering Medicinal Chemistry VI symposium’ at Newcastle University on 12th June 2020.

The organising committee are grateful to all those companies and individuals who provided sponsorship for this ‘Free to Attend’ meeting, without which it would be difficult to hold.

The organising committee gratefully acknowledge the generosity of the MedChemComm editorial board who gave all prize awardees an RSC certificate and one year’s free e-subscription to RSC Medicinal Chemistry. They also would like to express their thanks to the following organisations for their generous sponsorship of this symposium: Astex, BioAscent Discovery, Charles River, Concept Life Sciences, Domainex, Evotec, Giblin Consulting, GlaxoSmithKline, Sosei Heptares Johnson & Johnson, NS-MC Consulting, Pfizer, Redbrick Molecular, Strem, Sygnature Discovery and Vernalis.

They also wish to acknowledge the generosity of the University of Cambridge who allowed us free use of the lecture theatre and facilities in the Department of Chemistry and the RSC Biological and Medicinal Chemistry Sector who underpinned this symposium financially as well as the efficient symposium secretariat support by Maggi Churchouse Events.

FRONTIERS IN MEDICINAL CHEMISTRY WITH CHEMICAL EPIGENETICS SESSION ORGANISED BY THE GERMAN MEDICINAL CHEMISTRY DIVISIONS OF GDCh AND DPhG

The German Chemical Society (GDCh) and the German Pharmaceutical Society (DPhG) cordially invite you to participate in the annual meeting on ´Frontiers in Medicinal Chemistry´ March 22-25, 2020, Freiburg, followed by the 3rd Chemical Epigenetics Meeting, March 25-27, 2020.

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 Chemical Proteomics – Activity based Protein Profiling, Macrocyclic and Covalent Inhibitors, Young Investigators, Novel Computational Methods, Epigenetics, and Highlights in Medicinal Chemistry and Case Studies.

The scientific program will include lectures and poster presentations. It is the goal of the organizers 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. The Frontiers of Medicinal Chemistry Conference is followed by the 3rd Chemical Epigenetics Meeting, March 25-27, 2020.

More information:

https://veranstaltungen.gdch.de/tms/frontend/index.cfm?l=9286&sp_id="2"

www.chemepi.org

NEWS FROM THE DIVISION MEDICINAL CHEMISTRY & CHEMICAL BIOLOGY, ROYAL NETHERLANDS CHEMICAL SOCIETY (KNCV-MCCB)

The KNCV Division Medicinal Chemistry of the Royal Netherlands Chemical Society is happy to announce that they will proceed under a new name ‘Medicinal Chemistry & Chemical Biology’ (MCBB).

Given the interfaces and complementarities between medicinal chemistry and chemical biology, the division intends to represent both activities. Hereby, the division can improve its outreach and make a bigger impact on science and society. Importantly, the new name gives the excellent chemical biology research in The Netherlands a dedicated KNCV platform. These developments are also in line with ongoing efforts of the EFMC to broaden its scope.

The proud history and promising future of the division will be celebrated during our 50th anniversary symposium ‘A joint future for Medicinal Chemistry and Chemical Biology in the Netherlands’, in Eindhoven, 23-24 March 2020. https://farmacochemie.kncv.nl/mccb2020

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

The BMCS is pleased to announce some upcoming events.

ANGLO-SWISS SYMPOSIUM: USING CHEMICAL BIOLOGY TO IDENTIFY NEW TARGETS FOR MEDICINAL CHEMISTRY
4th February 2020, PharmaCenter, Basel, Switzerland
The call for poster abstracts will close 13th January 2020
Website: http://www.rsc.org/events/detail/41974/2nd-anglo-swiss-symposium-2020-using-chemical-biology-to-identify-new-targets-for-medicinal-chemistry

Synopsis: Experts in chemical biology and medicinal chemistry come to the scientific hub of Basel for a symposium featuring 8 speakers and a poster session. Exciting science is promised, as well as great networking opportunities.

2nd RSC/SCI APPLIED LATE STAGE FUNCTIONALISATION SYMPOSIUM
18th to 19th February 2020, University of Manchester, Manchester, UK
Website: http://www.rsc.org/events/detail/41281/applied-late-stage-functionalisation-where-chemistry-meets-biology

Synopsis: The meeting will highlight some of the hot and emerging developments in the inorganic catalysis and biocatalysis arenas and both the academic and application of late-stage functionalisation methodologies.

6th RSC/SCI SYMPOSIUM ON ION CHANNELS AS THERAPEUTIC TARGETS
24th to 25th February 2020, Wellcome Genome Campus Conference Centre, Cambridge, UK
Website: http://www.rsc.org/events/detail/36598/6th-ion-channels-as-therapeutic-targets

Synopsis: The symposium will showcase the most recent advances in ion channel science and promote scientific interaction between scientists with a shared interest in the field of ion channel drug discovery. The conference will be organised around series of plenary lectures delivered by international leaders in ion channels science and drug discovery from academia and industry.

1st RSC BMCS SYNTHESIS IN DRUG DISCOVERY AND DEVELOPMENT SYMPOSIUM
27th March 2020, Eli Lilly, Windlesham, Surrey, UK
The call for poster abstracts will close on 30th January
Website: http://www.rsc.org/events/detail/39710/synthesis-in-drug-discovery-and-development

Synopsis: This symposium aims to highlight and celebrate the crucial role which synthetic organic chemistry plays in the success of small molecule drug discovery. The three main themes of the symposium will be:
• Innovative synthesis facilitating candidate discovery,
• Novel bioisosteres and methodology applicable to drug discovery
• Overcoming challenges of scale-up and process scale chemistry

EFMC SHORT COURSE ON NEW OPPORTUNITIES IN GPCR DRUG DISCOVERY: REGISTRATIONS ARE OPEN!

 

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