Synthesis and Characterizations of Novel bi-ligand TbEu(cpioa)phen Phosphors with High Quantum Efficiency for WLED Applications.

The hydrothermal method was employed to synthesize a novel bi-ligands LnMOF: Ln(cpioa)phen. The secondary ligand 1, 10-phen serves as a bridging agent to further facilitate energy transfer between Ln ions and the primary ligand Hcpioa. A comparison between Ln(cpioa) MOFs (Ln: Tb, Eu) and Ln(cpioa)phen MOFs (Ln: Tb, Eu) reveals that addition of the secondary ligand significantly improves the emission intensity by as high as almost 34 times.

Bruton's Tyrosine Kinase Inhibitors with Distinct Binding Modes Reveal Differential Functional Impact on B-Cell Receptor Signaling.

Small molecule inhibitors of Bruton's tyrosine kinase (BTK) have been approved for the treatment of multiple B-cell malignancies and are being evaluated for autoimmune and inflammatory diseases. Various BTK inhibitors (BTKi) have distinct potencies, selectivity profiles, and binding modes within the ATP-binding site. On the basis of the latter feature, BTKis can be classified into those that occupy the back-pocket, H3 pocket, and the hinge region only.

Combinatorial inhibition of Tec kinases BTK and ITK is beneficial in ameliorating murine sclerodermatous chronic graft versus host disease.

Graft-versus-host disease (GVHD) is the major factor limiting the widespread use of potentially curative allogeneic hematopoietic stem cell transplant (allo-HSCT). Chronic GVHD is characterized by the activation of alloreactive donor immune cells, especially B- and T-cells, leading to tissue damage and pathogenic fibrosis. In this study, we used highly specific next-generation inhibitors of ITK (PCYC-274), BTK (PCYC-804), and ibrutinib-like BTK/ITK inhibitors (PCYC-914 and PCYC-401) in the B10.

Synthesis and characterization of single-phase Tb/Eu doped metal-organic framework phosphors for warm light WLED applications.

A novel single-phase luminescent material, Ln@bio-MOF-1 (Ln: Tb and Eu), was synthesized by a facile hydrothermal method. The structural and luminescence characteristics of the MOF materials were studied in detail. The chromaticity of the as-prepared samples might be easily modulated using molar amounts of Tb and Eu.

Qiangli Wuhu mixture alleviates LPS-induced pneumonia by inhibiting the TLR4/NF-κB/NLRP3 pathway: a study based on network pharmacology.

Context: Qiangli Wuhu (QLWH) mixture is a concoction approved and registered by Ningxia Medical Products Administration. It has therapeutic effects on various types of pneumonia.

Objective: To clarify the mechanisms of QLWH in treating pneumonia.

Synthesis and Study on Ni-Co Phosphite/Activated Carbon Fabric Composited Materials with Controllable Nano-Structure for Hybrid Super-Capacitor Applications.

The advantage of low resistivity and inactive binders makes binder-free electrode an excellent candidate for high-performance energy devices. A simple hydrothermal method was used to fabricate M(HPO)(OH) (M: Ni and Co) (MHP) arrays combined with activated carbon fabric (ACF) without binder. The structures of MHP can be easily tuned from bouquets to nano-sheets by the concentration of NaHPO.

YO: Eu/PMMA hybrid film as a converter for enhanced harvesting of broadband solar-blind UV light.

At present, the most common materials for solar-blind UV light detectors are wide band-gap semiconductors, which generally have high requirements and complex methods for preparation. Ordinary semiconductor materials such as silicon, , and were industrialized, but they were excluded for direct harvest of solar-blind UV light due to their inability to absorb solar-blind light photons. Here, inorganic-organic hybrid film of :/ was used as a spectral converter to realize the detection of broadband solar-blind UV light by ordinary semiconductor, converting broadband solar-blind UV luminescence to visible luminescence based on down-conversion process, after which the visible luminescence was detected by the Si photo-resister.

Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).

A series of novel, highly potent, selective, and ATP-competitive mammalian target of rapamycin (mTOR) inhibitors based on a benzoxazepine scaffold have been identified. Lead optimization resulted in the discovery of inhibitors with low nanomolar activity and greater than 1000-fold selectivity over the closely related PI3K kinases. Compound 28 (XL388) inhibited cellular phosphorylation of mTOR complex 1 (p-p70S6K, pS6, and p-4E-BP1) and mTOR complex 2 (pAKT (S473)) substrates.

Discovery of XL888: a novel tropane-derived small molecule inhibitor of HSP90.

With structural guidance, tropane-derived HTS hits were modified to optimize for HSP90 inhibition and a desirable in vivo profile. Through an iterative SAR development process 12i (XL888) was discovered and shown to reduce HSP90 client protein content in PD studies. Furthermore, efficacy experiments performed in a NCI-N87 mouse xenograft model demonstrated tumor regression in some dosing regimens.

Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase γ inhibitors.

The phosphoinositide 3-kinases (PI3Ks) have been linked to an extraordinarily diversified group of cellular functions making these enzymes compelling targets for the treatment of disease. A large body of evidence has linked PI3Kγ to the modulation of autoimmune and inflammatory processes making it an intriguing target for drug discovery. Our high-throughput screening (HTS) campaign revealed two hits that were nominated for further optimization studies.

Preparation and the luminescent properties of Tb3+-doped Gd2O3 fluorescent nanofibers via electrospinning.

Tb(3+)-doped Gd(2)O(3) (Gd(2)O(3):Tb(3+)) nanofibers were prepared via a simple electrospinning technique using poly(ethylene oxide) (PEO) and rare-earth acetate tetrahydrates (Ln(CH(3)COO)(3)·4H(2)O (Ln = Gd, Tb)) as precursors. The obtained nanofibers have an average diameter of about 80 nm and are composed of pure cubic Gd(2)O(3) phase. A possible formation mechanism for the nanofibers is proposed on the basis of the experimental results, which reveals that PEO acts as the structure directing template during the whole electrospinning and subsequent calcination process.

Desymmetrization of enone-diones via rhodium-catalyzed diastereo- and enantioselective tandem conjugate addition-aldol cyclization.

Catalytic tandem conjugate addition-enolate trapping represents an effective strategy for the design of catalytic transformations that enable formation of multiple C-C bonds. Recently, using enantioselective rhodium-catalyzed conjugate addition methodology, we developed a catalytic tandem conjugate addition-aldol cyclization of keto-enones. Here, we report related desymmetrizations and parallel kinetic resolutions involving the use of diones as terminal electrophiles.

Diastereoselective cycloreductions and cycloadditions catalyzed by Co(dpm)(2)-silane (dpm = 2,2,6,6-tetramethylheptane-3,5-dionate): mechanism and partitioning of hydrometallative versus anion radical pathways.

In the presence of phenylsilane and 5 mol % cobalt(II) bis(2,2,6,6-tetramethylheptane-3,5-dionate), aryl-substituted monoenone monoaldehydes and bis(enones) undergo reductive cyclization to afford syn-aldol and anti-Michael products, respectively. For both aldol and Michael cycloreductions, five- and six-membered ring formation occurs in good yield with high levels of diastereoselectivity. Cycloreduction of monoenone monoaldehyde 1a in the presence of d(3)-phenylsilane reveals incorporation of a single deuterium at the enone beta-position as an equimolar mixture of epimers, inferring rapid isomerization of the kinetically formed cobalt enolate prior to cyclization.

Organocatalytic Michael cycloisomerization of bis(enones): the intramolecular Rauhut-Currier reaction.

The utilization of enones as latent enolates enables regioselective enolate formation from chemically robust presursors. In this communication, we report a catalytic Michael cycloisomerization of bis(enones) under Morita-Baylis-Hillman conditions. Upon exposure to 10 mol % tributylphosphine, bis(enone) substrates afford both five- and six-membered ring products.