Chemical method developed to improve drug discovery

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Researchers at the Moffitt Cancer Center have developed a novel reagent that improves the precision of drug synthesis. This innovative method, which is being Nature communicationintroduces a new sulfur-fluoride exchange reagent (SuFEx) that enables highly controlled production of important sulfur-based molecules, including sulfinamides, sulfonimidamides, and sulfoximines.

These compounds are indispensable in the pharmaceutical industry, but their synthesis with the required stereochemical fidelity has been challenging. The innovative reagent t-BuSF exploits strain release reactivity to achieve unprecedented levels of efficiency and selectivity, paving the way for more effective drug development and broader applications in medical research.

“Sulfur-based compounds, including those developed using the new methods, are known to have favorable physicochemical properties that make them ideal candidates for drug development,” said Justin M. Lopchuk, Ph.D., lead author and associate member of the Drug Discovery Department at Moffitt. “The ability to rapidly and stereochemically synthesize these compounds opens new opportunities for developing targeted therapies that more effectively target cancer cells while minimizing side effects.”

By exploiting the unique properties of the t-BuSF reagent, researchers have been able to explore previously inaccessible chemical regions within the sulfur family, particularly in the S(IV) and S(VI) oxidation states. This progress has led to the creation of over 70 new chemical compounds, many of which have immediate applications in medicinal chemistry and the development of new pharmaceutical compounds.

Lopchuk adds that this research has already been used to significantly improve the scalable synthesis of DFV890, an investigational Novartis drug currently in clinical trials for myeloid diseases at Moffitt and other sites.

Reference: Athawale PR, Shultz ZP, Saputo A, Hall YD, Lopchuk JM. Strain-release-controlled reactivity of a chiral SuFEx reagent provides stereocontrolled access to sulfinamides, sulfonimidamides, and sulfoximines. Nat-Kommun. 2024;15(1):7001. doi: 10.1038/s41467-024-51224-w

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