New Chemical Method Enhances Drug Discovery

Researchers at Moffitt Cancer Center have introduced an innovative reagent that improves the precision of drug synthesis. This method, detailed in Nature Communications, highlights a novel sulfur fluoride exchange (SuFEx) reagent. It facilitates the controlled production of important sulfur-based molecules, such as sulfinamides, sulfonimidamides, and sulfoximines.

These sulfur-based compounds play a crucial role in the pharmaceutical industry. However, synthesizing them with the necessary stereochemical accuracy has been challenging. The new reagent, t-BuSF, employs strain-release reactivity, achieving levels of efficiency and selectivity not previously reached. This advancement enables more effective drug development and expands possibilities in medical research.

Justin M. Lopchuk, Ph.D., who leads the research within the Drug Discovery Department, explained, "Sulfur-based compounds generated with these methods exhibit favorable physiochemical properties, making them attractive for drug development." He emphasized that rapidly synthesizing these compounds with stereochemical control opens avenues for designing targeted therapies. These therapies can better combat cancer cells while minimizing side effects.

Utilizing the distinct characteristics of the t-BuSF reagent allows researchers to investigate previously unreachable areas within sulfur chemistry. This includes insights into S(IV) and S(VI) oxidation states. As a result, they have produced over 70 new chemical compounds, many ready for application in medicinal chemistry and new pharmaceuticals.

Lopchuk notes that this research has considerably advanced the scalable synthesis of DFV890. This investigational compound, developed by Novartis, is currently undergoing clinical trials at Moffitt and other locations for treating myeloid diseases.

Earlier SSP wrote about the new insights into the aging immune system.