The STAT3 oncogene is a promising molecular target for the design of a new class of anticancer drugs. In this letter, we describe the design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as novel STAT3 inhibitors. Compound 3 binds to STAT3 with a K(i) value of 190nM and is a promising lead compound for further design and optimization.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2009.01.091 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Rational design and synthesis of atomically precise nanocluster-based nanocomposites: a step towards environmental catalysis.
Chem Commun (Camb)
January 2025
School of Chemistry, Indian Institute of Science Education and Research Thiruvananthapuram, Thiruvananthapuram, Kerala, 695551, India.
Atomically precise metal nanoclusters (NCs) and metal-organic frameworks (MOFs) possess distinct properties that can present challenges in certain applications. However, integrating these materials to create new composite functional materials has gained significant interest due to their unique characteristics through a range of applications, particularly in catalysis. Considering MOFs as hosts and NCs as guests, several synergistic effects have been observed in composites, particularly in environmental catalytic reactions.
View Article and Find Full Text PDFCan the supplementation of autolyzed yeast (Saccharomyces cerevisiae) affect the diet digestibility, feeding behavior, levels of blood metabolites, and performance of Dorper × Santa Ines lambs finished in feedlot?
Trop Anim Health Prod
January 2025
Animal Science Department, Federal University of Paraná, Palotina, PR, 85950-000, Brazil.
This study aimed to evaluate the effect of autolyzed yeast (obtained from culture of Saccharomyces cerevisiae in sugarcane derivatives) supplementation on diet digestibility, feeding behavior, levels of blood metabolites associated with protein and energy metabolism, and performance of Dorper × Santa Ines lambs finished in feedlot. Twenty-four non-castrated male lambs with an average age of 4 months and a body weight (BW) of 19.49 ± 3.
View Article and Find Full Text PDFNeutral and ionic Co(II) metal-organic frameworks with 2-methylimidazole and trimesate: design and evaluation for molecule encapsulation and slow release.
Dalton Trans
January 2025
Deutsches Elektronen-Synchrotron DESY, Notkestr. 85, 22607 Hamburg, Germany.
Two Co(II) mixed-ligand metal-organic frameworks (MOFs) based on 2-methylimidazole and trimesate were synthesised at room temperature. The structure and properties of the two MOFs, named material Deutsches Elektronen Synchrotron-1 and -2 (mDESY-1 and mDESY-2), were verified by single crystal X-ray diffraction (SCXRD), powder X-ray diffraction (PXRD), SQUID magnetic susceptibility and N adsorption. The structural analysis indicates that mDESY-1 is a 3D ionic framework with 2-methyl-1-imidazol-3-ium counterions residing in its pores, while mDESY-2 is a 2D neutral framework isostructural to ITH-1, with water as a co-crystallising solvent.
View Article and Find Full Text PDFThe Impact of Ligand Structure and Reaction Temperature on Ethenolysis of Fatty Acid Methyl Esters Catalyzed by Spirocyclic Alkyl Amino Carbene Ru Complexes.
ChemSusChem
January 2025
Lomonosov Moscow State University: Moskovskij gosudarstvennyj universitet imeni M V Lomonosova, Department of Chemistry, Leninskie Gory, 1-3, 119991, Moscow, RUSSIAN FEDERATION.
Spirocyclic alkyl amino carbene (SCAAC) Ru complexes demonstrate outstanding activity and selectivity in ethenolysis of methyl oleate (MO) or fatty acid methyl esters (FAMEs), and 5,6-dimethoxyindane derivative was the most active catalyst to date. For the further catalyst design, we proposed modifying the spirocyclic fragment by fusion of saturated carbo- or heterocycle, linked to the 5,6-positions of indane or 6,7- positions of tetralin. Another suggested way of the modification of SCAAC complex was the insertion of chromane fragment to the carbene ligand.
View Article and Find Full Text PDFHost-Matrix Interactions and Molecular Functionalization: Shaping the Delayed Emission Properties of Indenophenanthridine Derivatives.
Chempluschem
January 2025
Lodz University of Technology, Molecular Physics, Faculty of Chemistry, POLAND.
The advancement of organic room temperature phosphorescence (RTP) materials has attracted considerable interest owing to their extensive applications. Their distinct advantages, including a metal-free composition, low toxicity, and facile synthesis under ambient conditions, make them highly desirable. This study examines the delayed fluorescence (DF) and RTP of metal-free, amorphous indenophenanthridine (IND)-based derivatives (1-10) and provides insights into molecular functionalisation and host matrix effects on delayed emission (RTP and DF).
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!