Solid-phase synthesis of imidazolyl-beta-amino acid derivatives is described. Several analogs demonstrated moderate inhibition of geranylgeranyl protein transferase type I (GGPT I).
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.bmcl.2005.01.042 | DOI Listing |
J Med Chem
January 2025
Department of Pharmaceutical and Cell Biological Chemistry, Pharmaceutical Institute, University of Bonn institution, An der Immenburg 4, Bonn 53121, Germany.
Targeted protein degradation (TPD) represents a promising alternative to conventional occupancy-driven protein inhibition. Despite the existence of more than 600 E3 ligases in the human proteome, so far only a few have been utilized for TPD of histone deacetylases (HDACs), which represent important epigenetic anticancer drug targets. In this study, we disclose the first-in-class Fem-1 homologue B (FEM1B)-recruiting HDAC degraders.
View Article and Find Full Text PDFDalton Trans
January 2025
Institute of Chemistry, St Petersburg University, Universitetskii pr. 26, 198504 St. Petersburg, Russia.
A series of cyclometalated Au(III) complexes [Au(C^N^C)(C-L-P(O)Ph)] with C^N^C = 2,6-diphenylpyridine and alkynylphosphine oxide ligands (L = no linker, Au1; phenyl, Au2; biphenyl, Au3; naphthyl, Au4; anthracenyl, Au5) were synthesized and fully characterized by spectroscopic methods and single crystal XRD analysis. The complexes obtained exhibit triplet (Au1-Au3) and dual (Au4, Au5) emissions in solution, in the solid phase and in the PMMA film, whose characteristics depend on the linker's nature of the alkynylphosphine oxide ligand. The description of electronic transitions responsible for energy absorption and emission in Au(III) complexes was made on the basis of a detailed analysis of the results of DFT calculations and has shown to involve ILCT, LLCT and MLCT transitions of singlet and triplet nature.
View Article and Find Full Text PDFACS Mater Au
January 2025
Materials Department, University of California Santa Barbara, California 93106, United States.
Of the few weberite-type Na-ion cathodes explored to date, NaFeF exhibits the best performance, with capacities up to 184 mAh/g and energy densities up to 550 Wh/kg reported for this material. However, the development of robust structure-property relationships for this material is complicated by its tendency to form as a mixture of metastable polymorphs, and transform to a lower-energy Na FeF perovskite compound during electrochemical cycling. Our first-principles-guided exploration of Fe-based weberite solid solutions with redox-inactive Mg and Al predicts an enhanced thermodynamic stability of NaMg Fe F as the Mg content is increased, and the = 0.
View Article and Find Full Text PDFToxicon
January 2025
Applied Immunology and Morphology Research Centre, NuPMIA, Morphology Area, Faculty of Medicine, University of Brasília, UnB, Brasília, Distrito Federal, Brazil. Electronic address:
Amphibian skin is a rich source of molecules with biotechnological potential, including the tryptophyllin family of peptides. Here, we report the identification and characterization of two tryptophyllin peptides, FPPEWISR and FPWLLS-NH, from the skin of the Central Dwarf Frog, Physalaemus centralis. These peptides were identified through cDNA cloning and sequence comparison.
View Article and Find Full Text PDFJ Fluoresc
January 2025
Department of Physics, R. T. M. Nagpur University, 440033, Nagpur, India.
The preparation of new phosphor with outstanding luminescent properties for white light-emitting diodes (WLEDs) is consistently a challenging. Here in the present study, A novel white-emitting chloropatite phosphor Ca(PO)Cl:Eu was synthesized via the pechini sol gel synthesis with citric acid and polyethylene glycol (PEG) acid as a fuel at 850 °C systematically investigating the impact of doping concentration and synthesis temperature on both photoluminescence properties and crystal phase. The structural characteristics and crystalline nature of the prepared sample were investigated by using X-ray diffraction (XRD) patterns and Fourier transform infrared (FT-IR) spectra.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!