Lead Diversification 2: application to P38, gMTP and lead compounds

Area of Science:

• Medicinal Chemistry
• Organic Synthesis
• Drug Discovery

Background:

• Drug discovery requires efficient methods for modifying molecular structures.
• C-H activation offers a powerful approach for targeted functionalization of drug candidates.
• Pfizer has developed a new technology platform to leverage these advancements.

Purpose of the Study:

• To introduce the Lead Diversification technology platform.
• To demonstrate the application of Lead Diversification in drug discovery programs.
• To report the development of novel screening assays for drug development.

Main Methods:

• Utilized C-H activation for the functionalization of drug molecules.
• Applied the Lead Diversification platform to specific drug programs (e.g., P38, gMTP).
• Developed new plate-based screening assays, including a fluorination screen.

Main Results:

• Successfully functionalized drug molecules using the Lead Diversification platform.
• Demonstrated the utility of the platform in advancing drug programs.
• Established novel screening methods for evaluating drug candidates.

Conclusions:

• Lead Diversification is a viable technology for drug molecule functionalization.
• The platform shows promise for accelerating drug discovery and development.
• New screening capabilities enhance the evaluation of novel drug candidates.