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ur group's research interests are in the areas of organophosphorus chemistry, and bioorganic/medicinal chemistry. The element phosphorus is the common thread throughout our research projects. The core of our program in phosphorus-based chemical biology focuses on the mechanism-based design, synthesis and evaluation of biologically active molecules such as enzyme inhibitors, and the development of novel antisense oligonucleotides with emphasis on the application of automated synthesis and combinatorial techniques whenever possible. Unnatural compounds are synthesized to probe various biological processes. Applications of this research range from the elucidation of enzyme mechanisms to the preparation of molecules with potential medicinal use (anticancer, antiparasite, immuno suppressant, antisense, GABA analogues). One such medicinally oriented goal is the preparation and evaluation of new hydrolytically stable “antisense oligonucleotides” for sequence specific complexation to RNA and DNA targets (such as peptide nucleic acids (PNAs)/phosphinate hybrids). We are also interested in 1,1-bisphosphorus compounds as pyrophosphate analogs, since pyrophosphate has a rich biochemical role. Finally, other investigations aiming at the modulation of GABA receptors with phosphinic analogues are relevant to the treatment of various central nervous system (CNS) disorders. With TCU’s Professor Coffer, we have also been preparing and evaluating components for biocompatible calcified nanoporous. In general, because phosphorus compounds are ubiquitous in living systems, the synthesis of phosphorus-containing mimics can have important medicinal benefits. Our second research interest concerns organophosphorus chemistry and is driven by several main objectives: firstly, the development of P-chiral ligands to be ultimately used in catalytic asymmetric transformations, including transition metal-catalyzed reactions; secondly, the building of a methodology to produce phosphorus compounds in general; and thirdly, the preparation of compounds possessing potential biological activity. Our expertise lies in the area of hypophosphorous compounds and their derivatives (H-phosphinates and phosphinates, and to a lesser extent phosphonates). One area of significant current interest in the laboratory, is the development of sustainable synthetic methodologies to avoid phosphorus trichloride (PCl3). Our program toward the development of new methodology for the synthesis of phosphinic acids has led to many novel reactions, including the palladium-catalyzed cross-coupling of hypophosphite derivatives with aryl, benzylic, and alkenyl electrophiles, and the room temperature radical addition of hypophosphites to olefins. These reactions are also applied to the synthesis of biologically active compounds, to the preparation of intermediates with industrial value, and to the preparation of P-chiral building blocks. Combining the above research directions into the same program provides valuable advantages. Because phosphorus is ubiquitous in nature, a variety of molecules can be designed to achieve some specific biological effect. To achieve the efficient synthesis of such compounds, new synthetic routes are required, which borrow from independently developed methodologies. In general, a combination of organic synthesis, methodology, and chemical biology, is used to pursue our objectives.
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The Cambridge Structural Database (2021)
PURE AND APPLIED CHEMISTRYno. 1 (2019): 113-120
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#Papers: 125
#Citation: 3971
H-Index: 35
G-Index: 61
Sociability: 5
Diversity: 0
Activity: 0
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