Synthesis in Drug Discovery and Development

 

Monday & Tuesday, 22nd & 23rd March 2021

(two afternoon sessions)

 

A virtual event

 

Registration is now closed

Registration closed at 12.00 GMT on Thursday, 18th March

 

Twitter hashtag #SDDD21

 

Downloads and Links

Second announcement and call for posters

First announcement

 

Flash presentation programme

Catalogue of posters

Twitter link to actual posters - no Twitter account is required

 

RSC special offer on affiliate membership - follow this link to see below

Link to the BMCS's COVID-19 statement

 

RSC website

 

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. Densely functionalised small molecules with a high degree of synthetic complexity are often the result of these demands. Successful programmes therefore 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 aimed to celebrate the crucial role of synthesis in the success of drug discovery and development.

 

GoToWebinar - hosting symposium

Grapevine - networking and meeting poster presenters, speakers, exhibitors and other registered delegates (open 11.00-13.00 and16.00-18.00 both days)

Twitter - hosting actual posters

 

Programme Themes and Features

The three main themes of the symposium were:
• Innovative synthesis facilitating candidate discovery
• Novel bioisosteres and methodology applicable to drug discovery
• Overcoming challenges of scale-up and process scale chemistry

 

Who should attend
Chemists from industry and academia, including synthetic, medicinal and process chemists.

 

Call for Posters
Applications were invited for poster presentation. Posters were displayed throughout both days and applicants were asked if they wished to provide a two-minute flash oral presentation when submitting their abstracts. The abstract closing date was 29th January.

 

A prize was awarded to the poster judged to be the best, a £100 RSC book voucher, kindly provided by "RSC Medicinal Chemistry Journal".   The winner was Angus McMillan of ETH Zürich, with his poster entitled "Sp3-rich virtual library construction and automated hit synthesis".   Well done, Angus!

 

Flash presentation programme

Catalogue of posters

Twitter link to actual posters - no Twitter account is required

 

Programme

Note:  All timings were UK time (GMT).

Where the presentation title appears in this colour, you may view a .pdf of the presentation slides.

 

Monday, 22nd March

13.00

Opening remarks

Duncan Hay, Vertex

 

 

Session chair:  Martin Swarbrick, Cancer Research UK

13.05

Innovative synthetic methods and their application to the discovery of ATAD2 inhibitors
Carine Guérot, AstraZeneca

13.45

Discovery, application and conformational bias of aryl 3-oxabicyclo[4.1.0]heptanes, non-nitrogen containing bioisosteres of N-aryl morpholines
Heather Hobbs and Luke Green, GlaxoSmithKline

14.25

Bioisosteric replacements and scale-up challenges in drug discovery

Thomas Fessard, SpiroChem

15.05

Refreshment break

 

 Session chair:  Nadia Ahmad, Charles River

15.20

Flash poster presentations (part 1) - download programme here

15.20Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood–brain barrier permeability
Chiara Borsari, University of Basel, Switzerland (P01)
15.22Synthesis of α-methyl-β- (N-piperidyl)propanoic acid hydrazide derivatives and their pharmacological activity
Dmitriy Berillo, University of Brighton, UK (P02)
15.24Catalytic α-C–H functionalisation of primary amines
Alexander Cresswell, University of Bath, UK (P03)
15.2Development of inhibitors for DNA gyrase as novel antibacterials
Kyle Orritt, University of Leeds, UK (P10)
15.28Studies towards the synthesis of functionalised bi-aryl drug candidates as ubiquitin ligase inhibitors
Joshua Hall, University of East Anglia, UK (P11)
15.30Synthesis of new DHEA 17-spiro-cyclopropyl derivatives with neurotrophic, neuroprotective and anti-inflammatory activity
Alessia Latorrata, National Hellenic Research Foundation, Greece (P16)

15.35

Development and application of facile and flexible 2+2+2 cyclo-trimerisation methodology and its impact on two lead identification programmes
Simon Peace, GlaxoSmithKline

16.15

New synthetic chemistry for the exploration of 3-D pharmaceutical space
Peter O'Brien, University of York

16.55Closing remarks

17.00

Networking with exhibitors, poster presenters and speakers

You were encouraged to join this networking session

17.45

Close

 

Tuesday, 23rd March

13.00

Opening remarks

Duncan Hay, Vertex

 

 

Session chair:  Katherine Jones, GlaxoSmithKline

13.05

Synthesis of new chemical motifs as design options for drug discovery

James Bull, Imperial College London

13.45

Glucose responsive insulin – synthesis enabling discovery and development

Paul Bulger, MSD

14.25

Modern organic synthesis in the discovery of chemical probes for new targets
Paul Brennan, Structural Genomics Consortium

15.05

Refreshment break

 

 Session chair:  Andrew Williams, Honorary Chairman of the RSC BMCS

15.20

Flash poster presentations (part 2) - download programme here
15.20Chiral resolution of anti-cancer β-lactam racemic derivatives of Combretastatin A-4 using column chromatography
Eavan McLoughlin, Trinity College, Dublin, Ireland (P05)
15.22Sp3-rich virtual library construction and automated hit synthesis
Angus McMillan, ETH Zürich, Switzerland (P06)
15.24Development of small molecule notum inhibitors to potentiate Wnt signalling
Hannah Woodward, University College London, UK (P09)
15.26Discovery of novel pyrimidine-based inhibitors of Respiratory Syncytial Virus fusion protein
Matthew Barrett, ReViral Ltd, UK (P13)
15.28New cannabinoid CB2 receptor modulators in the treatment of microglial-mediated neuroinflammation
Rebecca Ferrisi, University of Pisa, Italy (P14
(
15.30Novel continuous flow methodologies for the fast and effective generation of a new HBV inhibitor series
Justine Raymond, Institute of Chemical Research of Catalonia (ICIQ), Spain (P15)

15.35

Sp3-rich cyclic hydrazine frameworks for drug discovery

Mike Shipman, University of Warwick

16.15

A 3-way BET to scale up a trans-disubstituted dihydrobenzofuran active bromodomain inhibitor
Catherine Alder, GlaxoSmithKline

16.55

Closing remarks

17.00

Networking with exhibitors, poster presenters and speakers

You were encouraged to join this networking session

17.45

Close

 

Registration
Registration closed at 12.00 GMT on Thursday, 18th March

Registration fees were:

£50   RSC member*

£75   Non-member

£25   RSC student** member

£37   Student** non-member

 

* Member is paid-up member of the RSC.
** Student is undergraduate or post-graduate, not post-doc, and does not apply to students in paid employment.
 

Cancellation Policy
In the event of cancellation before 6th March 2021, 80% of the fee paid will be refunded. Cancellations must be received in writing. Refunds will not be possible from 7th March onwards, although substitutions are possible at any time.

In the unlikely event of cancellation of the meeting, fees paid will be refunded in full.

 

Exhibitor Opportunities
We were offering two alternative packages to our valued supporters.

 

Exhibitor Sponsorship Package
Charge of £60 and comprising:

- your name and weblink on this event webpage
- your logo in the rolling slides shown at the event and a web-linked logo in the electronic delegate handbook
- an A4 promotional page in the electronic delegate handbook
No delegate registration is included

Speaker Sponsorship Package
Charge of £120 and comprising:

- all features in the above Exhibitor Sponsorship Package, plus:
- a promotional slide shown before one talk or poster session
- your organisation’s name mentioned by the Session Chair prior to the presenter’s introduction

No delegate registration was included.

 

Confirmed Speaker Sponsors, with weblinks

Apex Molecular

BioAscent Discovery

BLD Pharmatech

Enantia

Charnwood Molecular

Liverpool ChiroChem

 

Confirmed Exhibitor Sponsors, with weblinks
Biotage AB, from Sweden

Enamine

ICB Nuvisan

Reach Separations

 

RSC Special Offer on Membership

 

 

We know that not everyone in the audience is a member of the Royal Society of Chemistry and there may be several reasons for this, but right now the RSC are offering free Affiliate membership to anyone who attends one of our online events. If you have ever considered joining but haven’t got around to it, or are not sure what you could get out of being a member, then maybe now is the time to sign up as an Affiliate for free and try it out.

Affiliate membership does not need a degree transcript or CV, simply go to rsc.li/affiliate and use the discount code IG100 to join - you can then become a member of our Interest Group, the BMCS, and keep up to date with all of our events and activities!

Affiliate membership offers:
- Free membership of one Interest Group*
- Depending on where you are in the world, automatic membership of an RSC Local Section

- Ten free RSC journal article downloads a year, and 35% off RSC books
- Online access to Chemistry World
- Access to careers resources and webinars, and discounts for accredited training courses
- Support from the Chemists’ Community Fund
- Discounts on travel, insurance, lifestyle and publications.
* You may wish to choose the BMCS (Biological and Medicinal Chemistry Sector)!

 

Sponsors
We are grateful to the organisations below for sponsoring this event.

 

 

 

 

 


We are grateful to our supporters below:

        

 

 

 

Organising Committee
Nadia Ahmad, Charles River
Duncan Hay (chair), Vertex
Martin Swarbrick (treasurer), Cancer Research UK
Andrew Williams, Hon Chairman, RSC BMCS

 

Secretariat Contact
Maggi Churchouse, 3 East Barn, Market Weston Road, Thelnetham, Diss IP22 1JJ, UK
Telephone: +44 (0)1359 221004
E-mail:  maggi@maggichurchouseevents.co.uk

 

Image credit
The image is derived from “Gilbert Chemistry Set” (https://tinyurl.com/y4smxepk) by Steve Lodefink, under CC BY (https://creativecommons.org/licenses/by/2.0)

 

Registration is now closed

 

Link to return to the RSC BMCS index page