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Subtle Structural Modifications Spanning from EP4 Antagonism to EP2/EP4 Dual Antagonism: A Novel Class of Thienocyclic-Based Derivatives.
J Med Chem
January 2025
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai 200241, China.
The development of dual prostaglandin E receptors 2/4 (EP2/EP4) antagonists represents an attractive strategy for cancer immunotherapy. Herein, a series of 4,7-dihydro-5-thieno[2,3-]pyran derivatives with potent EP2/EP4 dual antagonism were discovered by fine-tuned structural modifications. The biphenyl side chain was found to be the key pharmacophore for the transition from EP4 antagonism to EP2/EP4 dual antagonism.
View Article and Find Full Text PDFIsostructural Dy(III) and Er(III) complexes [L12Ln(H2O)5][I]3·L12·(CH2Cl2) (Ln = Dy (1), Er (3)) and [L22Ln(H2O)5][I]3·L22·(CH2Cl2)2 (Ln = Dy (2), Er (4)), with distorted pentagonal bipyramidal geometry (D5h) around the central metal were synthesized by utilizing two bulky phosphonamide ligands, adamantyl phosphonamide, (Ad)P(O)(NHiPr)2 (L1) and carbazolyl phosphoramide (Cz)P(O)(NHiPr)2 (L2). The resultant complexes were investigated for their magnetic properties in order to elucidate the impact of modification of the coordinating P-O bond environment either by increasing steric bulk and/or introduction of a third P-N bond at the central phosphorus atom. Magnetic studies revealed substantial energy barriers (Ueff) of 640 K and 560 K for Dy compounds 1 and 2, respectively, rendering them as some of the best-performing air-stable SIMs amongst the class of SIMs with D5h symmetry.
View Article and Find Full Text PDFAccurate stacking engineering of MOF nanosheets as membranes for precise H sieving.
Nat Commun
December 2024
Beijing Key Laboratory for Membrane Materials and Engineering, Department of Chemical Engineering, Tsinghua University, Beijing, 100084, China.
Two-dimensional (2D) metal-organic framework (MOF) nanosheet membranes hold promise for exact molecular transfer due to their structural diversity and well-defined in-plane nanochannels. However, achieving precise regulation of stacking modes between neighboring nanosheets in membrane applications and understanding its influence on separation performance remains unrevealed and challenging. Here, we propose a strategy for accurately controlling the stacking modes of MOF nanosheets via linker polarity regulation.
View Article and Find Full Text PDFAchieving Linear α-Macro-olefins in Ethylene Polymerization through Precisely Tuned Bis(imino)pyridylcobalt Precatalysts with Steric and Electronic Parameters.
Precis Chem
December 2024
Key Laboratory of Engineering Plastics and Beijing National Laboratory for Molecular Science, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China.
Synthesis of functional polyethylene from ethylene alone is tricky and heavily dependent on both the type and structure of the precatalyst and the choice of cocatalyst used in the polymerization. In the present study, a series of cobalt precatalysts was prepared and investigated for ethylene polymerization under various conditions. By incorporation of strong electron-withdrawing groups (F and NO) and a steric component (benzhydryl) into the parent bis(imino)pyridine ligand, the catalytic performance of these precatalysts was optimized.
View Article and Find Full Text PDFTuning steric hindrance of cyclic ether electrolytes enables high-voltage lithium metal batteries.
J Colloid Interface Sci
December 2024
School of Materials Science and Engineering, Key Laboratory of Green Fabrication and Surface Technology of Advanced Metal Materials of Ministry of Education, Anhui University of Technology, Maanshan 243002, China; Key Laboratory of Efficient Conversion and Solid-state Storage of Hydrogen & Electricity of Anhui Province, Maanshan 243002, China. Electronic address:
Ether-based electrolytes are known for their high stability with lithium metal anodes (LMAs), but they often exhibit poor high-voltage stability. Structural optimization of ether-based solvent molecules has been proven to effectively broaden the electrochemical window of these electrolytes, yet the optimization rules within cyclic ethers remain unclear. Herein, we investigate the impact of methyl substitution positions on the molecular properties of 1,3-dioxolane (DOL), a commonly used cyclic ether.
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