Month: October 2022

Anson, Francesca; Kanjilal, Pintu; Thayumanavan, S.; Hardy, Jeanne A. published the artcile< Tracking exogenous intracellular casp-3 using split GFP>, Reference of 2127-03-9, the main research area is green fluorescent protein exogenous intracellular caspase cytosol; apoptosis; caspase; caspase-3; intracellular protein delivery; nanogel; split GFP.

Cytosolic protein delivery promises diverse applications from therapeutics, to genetic modification and precision research tools. To achieve effective cellular and subcellular delivery, approaches that allow protein visualization and accurate localization with greater sensitivity are essential. Fluorescently tagging proteins allows detection, tracking and visualization in cellulo. However, undesired consequences from fluorophores or fluorescent protein tags, such as nonspecific interactions and high background or perturbation to native protein””s size and structure, are frequently observed, or more troublingly, overlooked. Distinguishing cytosolically released mols. from those that are endosomally entrapped upon cellular uptake is particularly challenging and is often complicated by the inherent pH-sensitive and hydrophobic properties of the fluorophore. Monitoring localization is more complex in delivery of proteins with inherent protein-modifying activities like proteases, transacetylases, kinases, etc. Proteases are among the toughest cargos due to their inherent propensity for self-proteolysis. To implement a reliable, but functionally silent, tagging technol. in a protease, we have developed a caspase-3 variant tagged with the 11th strand of GFP that retains both enzymic activity and structural characteristics of wild-type caspase-3. Only in the presence of cytosolic GFP strands 1-10 will the tagged caspase-3 generate fluorescence to signal a non-endosomal location. This methodol. facilitates easy screening of cytosolic vs. endosomally-entrapped proteins due to low probabilities for false pos. results, and further, allows tracking of the resultant cargo′s translocation. The development of this tagged casp-3 cytosolic reporter lays the foundation to probe caspase therapeutic properties, charge-property relationships governing successful escape, and the precise number of caspases required for apoptotic cell death.

Protein Science published new progress about Affinity tags Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Reference of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Winter, Andreas; Endres, Patrick; Schroeter, Erik; Jaeger, Michael; Goerls, Helmar; Neumann, Christof; Turchanin, Andrey; Schubert, Ulrich S. published the artcile< Towards covalent photosensitizer-polyoxometalate dyads-bipyridyl-functionalized polyoxometalates and their transition metal complexes>, Computed Properties of 366-18-7, the main research area is hybrid materials; metal complexes; photocatalysis; polyoxometalates.

A triol-functionalized 2,2′-bipyridine (bpy) derivative has been synthesized and used for the tris-alkoxylation of polyoxometalate (POM) precursors. The resultant POM-bpy conjugates of the Wells-Dawson- and Anderson-type feature a C-C bond as a linkage between the POM and bpy fragments. This structural motif is expected to increase the hydrolytic stability of the compounds This is of particular relevance with respect to the application of POM-bpy metal complexes, as photocatalysts, in the hydrogen-evolution reaction (HER) in an aqueous environment. Accordingly, Rh(III) and Ir(III) complexes of the POM-bpy ligands have been prepared and characterized. These catalyst-photosensitizer dyads have been analyzed with respect to their electrochem. and photophys. properties. Cyclic and square-wave voltammetry, as well as UV/vis absorption and emission spectroscopy, indicated a negligible electronic interaction of the POM and metal-complex subunits in the ground state. However, emission-quenching experiments suggested an efficient intramol. electron-transfer process from the photo-excited metal centers to the POM units to account for the non-emissive nature of the dyads (thus, suggesting a strong interaction of the subunits in the excited state). In-depth photophys. investigations, as well as a functional characterization, i.e., the applicability in the HER reaction, are currently ongoing.

Molecules published new progress about 366-18-7. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Computed Properties of 366-18-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Morales-Colon, Maria T.; See, Yi Yang; Lee, So Jeong; Scott, Peter J. H.; Bland, Douglas C.; Sanford, Melanie S. published the artcile< Tetramethylammonium Fluoride Alcohol Adducts for SNAr Fluorination>, Recommanded Product: 4,4′-Dichloro-2,2′-bipyridine, the main research area is aryl chloride tetramethylammonium fluoride regioselective nucleophilic aromatic fluorination; aromatic fluoride preparation.

Nucleophilic aromatic fluorination (SNAr) is among the most common methods for the formation of C(sp2)-F bonds. Despite many recent advances, a long-standing limitation of these transformations was the requirement for rigorously dry, aprotic conditions to maintain the nucleophilicity of fluoride and suppress the generation of side products. This report addresses this challenge by leveraging tetramethylammonium fluoride alc. adducts (Me4NF·ROH) as fluoride sources for SNAr fluorination. Through systematic tuning of the alc. substituent (R), tetramethylammonium fluoride tert-amyl alc. (Me4NF·t-AmylOH) was identified as an inexpensive, practical, and bench-stable reagent for SNAr fluorination under mild and convenient conditions (80°C in DMSO, without the requirement for drying of reagents or solvent). A substrate scope of more than 50 (hetero) aryl halides and nitroarene electrophiles was demonstrated.

Organic Letters published new progress about Aryl bromides Role: RCT (Reactant), RACT (Reactant or Reagent). 1762-41-0 belongs to class pyridine-derivatives, and the molecular formula is C10H6Cl2N2, Recommanded Product: 4,4′-Dichloro-2,2′-bipyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Chen, Guihua; Cao, Jian; Wang, Qian; Zhu, Jieping published the artcile< Desymmetrization of Prochiral Cyclopentenes Enabled by Enantioselective Palladium-Catalyzed Oxidative Heck Reaction>, Formula: C13H15F3N2O, the main research area is desymmetrization cyclopentene enantioselective oxidative Heck palladium catalyst; oxidative Heck arylboronic acid cyclopentene palladium catalyst diastereoselective enantioselective.

In the presence of a catalytic amount of Pd(TFA)2 and a chiral Pyox ligand under oxygen atm., oxidative Heck reaction between arylboronic acids and 4-substituted or 4,4-disubstituted cyclopent-1-enes afforded the chiral arylated products with concurrent creation of two stereocenters in good yields with excellent diastereo- and enantioselectivities.

Organic Letters published new progress about Arylboronic acids Role: RCT (Reactant), RACT (Reactant or Reagent). 1416819-91-4 belongs to class pyridine-derivatives, and the molecular formula is C13H15F3N2O, Formula: C13H15F3N2O.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hai, Yang; Geng, Jia-Jia; Li, Peng-Jie; Ma, Wei-Ping; Wang, Cui-Fang; Wei, Mei-Yan; Hou, Xue-Mei; Chen, Guang-Ying; Gu, Yu-Cheng; Liu, Ming; Shao, Chang-Lun published the artcile< Semisynthesis and biological evaluation of (+)-sclerotiorin derivatives as antitumor agents for the treatment of hepatocellular carcinoma>, Recommanded Product: 3-(Aminomethyl)-6-(trifluoromethyl)pyridine, the main research area is hepatocellular cervical carcinoma sclerotiorin antitumor cytotoxicity pharmacokinetics signaling; (+)-Sclerotiorin; AKT and ERK proteins; Antitumor; Hepatocellular carcinoma; Mouse xenograft model.

Hepatocellular carcinoma is one of the most common primary hepatic malignancy. Herein, a series of semisynthesized derivatives (2-30) of the natural product (+)-sclerotiorin (1) was prepared and evaluated the cytotoxic activities against six cancer cell lines. Among them, 3 and 5 were the most effective compounds against human hepatocellular carcinoma Bel-7402 cell line with IC50 values of 1.45 and 1.15 μM, resp. Mol. mechanism study showed that 5 disrupted the mitochondrial membrane potential and induced apoptosis in a caspase-dependent manner. In addition, 5 affected AKT and ERK signaling pathways and induced AKT and ERK proteins degradation through ubiquitin-proteasome system. Furthermore, 5 displayed significant in vivo anticancer effects in the xenograft models with decreasing the tumor mass by 52.5%. The safety evaluation was confirmed by acute toxicity subchronic toxicity tests, paraffin sections of mice organ and blood routine examination Taken together, 5 can be developed as a potential therapeutic agent for hepatocellular carcinoma.

European Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 387350-39-2 belongs to class pyridine-derivatives, and the molecular formula is C7H7F3N2, Recommanded Product: 3-(Aminomethyl)-6-(trifluoromethyl)pyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Cheng, Kaiwu; Li, Yaojia; Gao, Zhiguo; Chen, Fanghui; You, Chaoqun; Sun, Baiwang published the artcile< Two-dimensional metal organic framework for effective gas absorption>, Safety of 2,4-Bipyridine, the main research area is soft phys exfoliation method preparation cadmium bipyridine MOF; crystal structure cadmium bipyridine MOF; gas adsorption thermal decomposition cadmium bipyridine MOF.

Herein, crystalline metal organic framework (MOF) nanosheets were fabricated through using a modified soft phys. exfoliation method from bulk crystals of a layered MOF, [Cd(4,4′-bpy)2(H2O)2](ClO4)2·(2,4′-bpy)2·H2O (MOF-1, 1), and fully characterized via transmission electron microscope (TEM), SEM, and at. force microscope (AFM). The delaminated MOF-1 nanosheets with porous structure showed good growth potential in selective gas adsorption.

Inorganic Chemistry Communications published new progress about Crystal structure. 581-47-5 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Safety of 2,4-Bipyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Rai, Roopa; Kolesnikov, Aleksandr; Sprengeler, Paul A.; Torkelson, Steven; Ton, Tony; Katz, Bradley A.; Yu, Christine; Hendrix, John; Shrader, William D.; Stephens, Robin; Cabuslay, Ronnell; Sanford, Ellen; Young, Wendy B. published the artcile< Discovery of novel heterocyclic factor VIIa inhibitors>, Category: pyridine-derivatives, the main research area is aminopyrrolopyridine preparation factor VIIa inhibitor SAR.

Structure-activity relationships and binding mode of novel heterocyclic factor VIIa inhibitors will be described. In these inhibitors, a highly basic 5-amidinoindole moiety has been successfully replaced with a less basic 5-aminopyrrolo[3,2-b]pyridine scaffold.

Bioorganic & Medicinal Chemistry Letters published new progress about Anticoagulants. 220731-04-4 belongs to class pyridine-derivatives, and the molecular formula is C10H15N3O2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

McCammant, Matthew S.; Sigman, Matthew S. published the artcile< Development and investigation of a site selective palladium-catalyzed 1,4-difunctionalization of isoprene using pyridine-oxazoline ligands>, Category: pyridine-derivatives, the main research area is pyridine oxazoline ligand preparation; polyene regioselective diastereoselective preparation; isoprene vinyl triflate vinylboronic acid palladium catalyst difunctionalization.

Palladium-catalyzed 1,4-difunctionalizations of isoprene that produce skipped polyenes were reported. Complex isomeric product mixtures were possible as a result of the difficult-to-control migratory insertion of isoprene into a Pd-alkenyl bond, but good site selectivity was achieved using easily accessible pyrox ligands. Mechanistic studies suggest that the control of insertion was the result of the unique electronic asymmetry and steric properties of the ligand.

Chemical Science published new progress about Addition reaction catalysts, stereoselective (regioselective). 1416819-91-4 belongs to class pyridine-derivatives, and the molecular formula is C13H15F3N2O, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Uraguchi, Daisuke; Kinoshita, Natsuko; Kizu, Tomohito; Ooi, Takashi published the artcile< Synergistic Catalysis of Ionic Bronsted Acid and Photosensitizer for a Redox Neutral Asymmetric α-Coupling of N-Arylaminomethanes with Aldimines>, COA of Formula: C33H21F3IrN3, the main research area is aldimine arylaminomethane chiral arylaminophosphonium iridium enantioselective coupling visible light; aryl diamine stereoselective preparation; chiral arylaminophosphonium photosensitizer iridium enantioselective coupling synergistic catalyst.

A redox neutral, highly enantioselective coupling between N-arylaminomethanes and N-sulfonyl aldimines was developed by harnessing the efficient catalysis of P-spiro chiral arylaminophosphonium barfate and a transition-metal photosensitizer under visible light irradiation This mode of synergistic catalysis provides a powerful strategy for controlling the bond-forming processes of reactive radical intermediates.

Journal of the American Chemical Society published new progress about Aldimines Role: RCT (Reactant), RACT (Reactant or Reagent). 370878-69-6 belongs to class pyridine-derivatives, and the molecular formula is C33H21F3IrN3, COA of Formula: C33H21F3IrN3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Connon, Stephen J.; Hegarty, Anthony F. published the artcile< Stabilized 2,3-pyridyne reactive intermediates of exceptional dienophilicity>, Product Details of C6H5BrClNO, the main research area is regioselective lithiation thiophenoxy chloropyridine; thiophenoxy pyridyne preparation; pyridine endoxide preparation.

The enhanced dienophilicity of 4-methoxy, 4-aryloxy and 4-thiophenoxy analogs of 2,3-pyridyne relative to itself is reported. The regioselective lithiation of 4-alkoxy- and 4-thiophenoxy-2-chloropyridine at low temperatures, followed by elimination of lithium chloride affords 4-alkoxy- and 4-thiophenoxypyridynes, which can be trapped in situ in a [4+2] cycloaddition reaction with furan to give endoxides in moderate to good yields (25-58%). In contrast, precursors with a hydrogen or Me substituent at C-4 give no evidence for pyridyne formation under these conditions. Attempts to generate 6-isopropoxy-2,3-pyridyne from the low-temperature lithiation of 2-chloro-6-isopropoxypyridine were unsuccessful due to the instability of the 2-chloro-6-isopropoxy-5-lithiopyridine.

European Journal of Organic Chemistry published new progress about [4+2] Cycloaddition reaction. 777931-67-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrClNO, Product Details of C6H5BrClNO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem