Bolm_Fergen_RWTH_DAV-AUT-7eb-3.pdf (62.6 KB) Bolm_Fergen_RWTH_DAV-AUT-7eb-3.modif.pdf (66.7 KB)
These set molecules - part of the DAV-AUT-7eb submission - are rather simple fragments and might be not sufficiently optimized to be tested in complex cell-based assays. I would de-prioritize the synthesis of this molecules, while putting a higher priority on the more complex cyclic sulfoximines reported in the DAV-AUT-7eb submission or the DAV-AUT-fa2 compounds.
Hello, thanks for your submission! We are currently ranking the designed molecules but due to their long synthesis (more than 4 steps) your complex molecules pass the makeability filter (ca 4 steps max)
Is your lab still operational and would you be willing to make them?
Anthony
Hi Anthony. More synthesis schemes for all compounds submitted (DAV-AUT series) are available. Prof. Bolm at RWTH Aachen University and his collaborators put massive efforts to provide the scientific community their input.
Hi Anthony. Update: Prof. Bolm’s lab. is not operational due to the recent measures to contain COVID-19. Synthetic schemes and help to carry out the reactions are available.
Ok thanks for checking. As an organic chemist the molecules you submitted are interesting, but challenging to synthesise. However, they might be submitted to a tier2 and offered to the global scientific community. If they are made, we will test them.
Hi Anthony. Thank you for your message.
As a team, we fully embraced the Moonshot principle. We designed advanced novel molecules, with a property range that we believe is suitable for assays involving more complex biological systems.
The design principles behind them is very robust, checked with several drug discovery scientists in big organizations.
I hope they will go forward in tier2. Please keep us updated and we are very happy to help you in the selection or lead-optimization process, if needed.