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Integrated Platform for Expedited Synthesis-Purification-Testing of Small Molecule Libraries
Aleksandra Baranczak1, Noah P Tu1, Jasmina Marjanovic1
1Discovery Chemistry and Technology, AbbVie Inc., 1 North Waukegan Road, North Chicago, Illinois 60064, United States.
ACS Medicinal Chemistry Letters
|April 25, 2017
Summary
Automated platforms accelerate medicinal chemistry by integrating synthesis, purification, and testing of small molecule libraries. This speeds up drug discovery cycles, enabling faster development of new therapeutics.
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Chemical Biology
Background:
- Medicinal chemistry programs face challenges in productivity and discovery cycle times.
- Automation offers a potential solution to enhance efficiency in small molecule library development.
Purpose of the Study:
- To describe a fully automated and integrated platform for small molecule library synthesis, purification, quantitation, dissolution, and testing.
- To validate the platform's performance and its impact on accelerating drug discovery cycles.
Main Methods:
- Development and implementation of an automated platform consolidating multiple chemistry workflows.
- Validation using synthesis and testing of two small molecule libraries targeting polycomb protein EED.
- Utilizing a broad array of chemical transformations for batch-supported compound synthesis.
Main Results:
- Excellent correlation between automated and conventional methods for library data generation.
- Achieved a library turnaround time of 24-36 hours.
- Generated sufficient compound quantities for secondary assays, significantly shortening discovery timelines.
Conclusions:
- The described automated platform substantially increases medicinal chemistry program productivity.
- This integrated system accelerates the discovery of small molecule therapeutics.
- The platform enables efficient synthesis and testing, reducing overall drug discovery cycle times.
