PhD Scientific Days 2025

EUniWell I.

UGI 3 component reaction for new classes of sulfoximine derivatives of potential biological activity

Name of the presenter

Splandesci Marta

Institute/workplace of the presenter

Medical University of Warsaw, Faculty of Pharmacy, Department of drug technology and pharmaceutical biotechnology

Authors

Marta Splandesci¹, Maciej Dawidowski¹

1: Medical University of Warsaw, Faculty of Pharmacy, Department of drug technology and pharmaceutical biotechnology

Text of the abstract

Sulfoximine is a chemical moiety that is of increasing interest in drug discovery. It is considered bioisosteric to e.g. sulfone, sulfonamide, secondary amine, hydroxyl, and carbonyls. It has an interesting reactivity and may contribute to achieving a desired pharmaco(chemical) properties of the target molecule, such as high aqueous solubility and metabolic stability(1). Consequently, sulfoximines may constitute promising leads for drug discovery and first compounds bearing this functional group are currently in clinical trials(2). Considering the desired properties of sulfoximines and the rich possibility of exploring novel chemistries around them, we investigate their possible use in obtaining biologically interesting derivatives through multicomponent reactions (MCRs), particularly the UGI three-component reaction (U-3CR)(3). We focus on the optimization of reaction conditions and on obtaining compound libraries of sulfoximine derivatives, which will be tested to evaluate their biological activity, and to highlight the usefulness of the applied synthetic methodology in medicinal chemistry and chemical biology. The results obtained may provide useful for the pharmaceutical industry and
researchers in the field of drug discovery.
References
1) Mäder P, et al. J. Med. Chem. 2020, 63, 14243–75
2) Melanie M. Frigault, et al. Cancer Research Communications, 2023, 3(11), 2268–2279
3) Cores A, et al. Pharmaceuticals 2022, 15, 1009

This project is funded by Polish National Science Center (NCN), OPUS24 grant, Reg. No. UMO-2022/47/B/NZ7/01411