Tag: M.W=200-250

Zhang, Lin; Fan, Junhua; Chong, Jer-Hong; Cesena, Angela; Tam, Betty Y. Y.; Gilson, Charles; Boykin, Christina; Wang, Deping; Aivazian, Dikran; Marcotte, Doug; Xiao, Guangqing; Le Brazidec, Jean-Yves; Piao, Jinhua; Lundgren, Karen; Hong, Kevin; Vu, Khang; Nguyen, Khanh; Gan, Liang-Shang; Silvian, Laura; Ling, Leona; Teng, Min; Reff, Mitchell; Takeda, Nicole; Timple, Noel; Wang, Qin; Morena, Ron; Khan, Samina; Zhao, Shuo; Li, Tony; Lee, Wen-Cherng; Taveras, Arthur G.; Chao, Jianhua published the artcile< Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I)>, Related Products of 220731-04-4, the main research area is pyrazolopyrimidine sulfonamide preparation multiple mitotic kinase inhibitor.

A novel class of pyrazolopyrimidine-sulfonamides was discovered as selective dual inhibitors of aurora kinase A (AKA) and cyclin-dependent kinase 1 (CDK1). These inhibitors were originally designed based on an early lead (compound I). SAR development has led to the discovery of potent inhibitors with single digit nM IC50s towards both AKA and CDK1. An exemplary compound II has demonstrated good efficacy in an HCT116 colon cancer xenograft model.

Bioorganic & Medicinal Chemistry Letters published new progress about Alkylation. 220731-04-4 belongs to class pyridine-derivatives, and the molecular formula is C10H15N3O2, Related Products of 220731-04-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Canakci, Mine; Singh, Khushboo; Munkhbat, Oyuntuya; Shanthalingam, Sudarvili; Mitra, Ankita; Gordon, Mallory; Osborne, Barbara A.; Thayumanavan, S. published the artcile< Targeting CD4+ Cells with Anti-CD4 Conjugated Mertansine-Loaded Nanogels>, Related Products of 2127-03-9, the main research area is tumor antitumor T cell antibody CD4 mertansine.

CD4+ T lymphocytes play an important role in controlling many malignancies. The modulation of CD4+ T cells through immunomodulatory or cytotoxic drugs could change the course of disease progression for disorders such as autoimmunity, immunodeficiency, and cancer. Here, we demonstrate that anti-CD4 conjugated polymeric nanogels can deliver a small mol. cargo to primary CD4+ T cells and a CD4high T cell lymphoma. The antibody conjugation not only increased the uptake efficiency of the nanogel (NG) by CD4+ T cells but also decreased the non-specific uptake of the NG by CD4- lymphocytes. For T lymphoma cell lines, the mertansine-loaded conjugate displayed a dose-dependent cell growth inhibition at 17 ng/mL antibody concentration On the other hand, antibody-drug conjugate (ADC)-type formulation of the anti-CD4 reached similar levels of cell growth inhibition only at the significantly higher concentration of 1.8μg/mL. NG and antibody conjugates have the advantage of carrying a large payload to a defined target in a more efficient manner as it needs far less antibody to achieve a similar outcome.

Biomacromolecules published new progress about Antibodies and Immunoglobulins Role: BPN (Biosynthetic Preparation), PAC (Pharmacological Activity), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses) (mertansine-polymer conjugates). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Related Products of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Xiao, Zhiwei; Wang, Lu; Wei, Junjie; Ran, Chongzhao; Liang, Steven H.; Shang, Jingjie; Chen, Guang-Ying; Zheng, Chao published the artcile< Visible-light induced decarboxylative coupling of redox-active esters with disulfides to construct C-S bonds>, Application In Synthesis of 2127-03-9, the main research area is aryldisulfide hydroxyphthalimide ester preparation ruthenium photocatalyst decarboxylative coupling; benzenethiosulfonate hydroxyphthalimide ester preparation ruthenium photocatalyst decarboxylative coupling; aryl thioether preparation.

A novel method was established for the construction of C-S bonds using redox-active esters with disulfides in the presence of Ru-photoredox catalyst. This method exhibited remarkable functional group tolerance across a wide scope of substrates. Under mild conditions, a structurally diverse array of aryl alkyl sulfides was successfully and efficiently obtained through decarboxylative cross-coupling.

Chemical Communications (Cambridge, United Kingdom) published new progress about Decarboxylation catalysts (photochem.). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Application In Synthesis of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

de Campos, Nathalia R.; Simosono, Cintia A.; Landre Rosa, Iara M.; da Silva, Rafaela M. R.; Doriguetto, Antonio C.; do Pim, Walace D.; Gomes Simoes, Tatiana R.; Valdo, Ana Karoline S. M.; Martins, Felipe T.; Sarmiento, Charlie V.; Nunes, Wallace C.; Guedes, Guilherme P.; Pedroso, Emerson F.; Pereira, Cynthia L. M.; Stumpf, Humberto O.; Lloret, Francesc; Julve, Miguel; Marinho, Maria Vanda published the artcile< Building-up host-guest helicate motifs and chains: a magneto-structural study of new field-induced cobalt-based single-ion magnets>, Electric Literature of 2127-03-9, the main research area is cobalt chloride hexahydrate dipyridyldisulfide magnetostructural correlation single ion magnet.

In this work, we present the synthetic pathway, a refined structural description, complete solid-state characterization and the magnetic properties of four new cobalt(II) compounds of formulas [Co(H2O)6][Co2(H2mpba)3]·2H2O·0.5dmso (1), [Co(H2O)6][Co2(H2mpba)3]·3H2O·0.5dpss (2), [Co2(H2mpba)2(H2O)4]n·4nH2O (3), and [Co2(H2mpba)2(CH3OH)2(H2O)2]n·0.5nH2O·2ndpss (4) [dpss = 2,2′-dipyridyldisulfide and H4mpba = 1,3-phenylenebis(oxamic) acid], where 2 and 4 were obtained from [Co(dpss)Cl2] (Pre-I) as the source of cobalt(II). All four compounds are air-stable and were prepared under ambient conditions. 1 and 2 were obtained from a slow diffusion method [cobalt(II) : H2mpba2- molar ratio used 1 : 1] and their structures are made up of [Co2(H2mpba)3]2- anionic helicate units and [Co(H2O)6]2+ cations, exhibiting supramol. three-dimensional structures. Interestingly, a supramol. honeycomb network between the helicate units interacting with each other through R22(10) type hydrogen bonds occurs in 2 hosting one co-crystallized dpss mol. On the other hand, for the first time, linear (3) and zigzag (4) cobalt(II) chains were isolated by slow evaporation of stirred solutions of mixed solvents with cobalt(II) : H2mpba2- in 1 : 2 molar ratio at room temperature Magnetic measurements of Pre-I revealed a quasi magnetically isolated S = 3/2 spin state with a significant second-order spin-orbit contribution as expected for tetrahedrally coordinated cobalt(II) ions. The anal. of the variable temperature static (dc) magnetic susceptibility data through first- (1 and 3) and second-order spin-orbit coupling models (2 and 4) reveals the presence of magnetically non-interacting high-spin cobalt(II) ions with easy-axis (1 and 4)/easy-plane magnetic anisotropies (2 and 4) with low rhombic distortions. Dynamic (ac) magnetic measurements for Pre-I and 1-4 below 8.0 K show that they are examples of field-induced Single-Ion Magnets (SIMs).

Dalton Transactions published new progress about Alternating current. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Electric Literature of 2127-03-9.

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

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

Li, Xuefu; Wang, Jun; Ba, Wanyu; Zhang, Suqiu; Lin, Zhenxian; Gao, Ming; Tian, Hua; Ru, Shaoguo published the artcile< Mechanistic revealing of reproductive behavior impairment in male guppy (Poecilia reticulata) induced by environmentally realistic 2,2'-dithiobis-pyridine exposure>, SDS of cas: 2127-03-9, the main research area is transcriptome dithiobis pyridine reproductive behavior impairment Poecilia; (PS)(2); Ecological safety; Mechanism study; Sexual behavior.

Although (PS)2, the primary degradation product of emerging antifouling biocides metal pyrithiones (MePTs), can disrupt the reproductive behavior of fish at an environmentally relevant ng/L level, the underlying mechanism is still largely unknown. This study exposed sexually mature male guppy (Poecilia reticulata) to 20, 200, and 2000 ng/L (PS)2 to explore the compromised effect of (PS)2 on reproductive behavior through a realistic competing scenario. The results showed that (PS)2 suppressed male guppies’ sexual interest to stimulus females, reduced their competitive behavior frequencies toward rival males, and decreased their mating time and frequency. (PS)2 exposure did not affect male guppies’ secondary sexual characteristics or induce estrogenic activity. Whole-brain transcriptome sequencing identified 1070 differentially expressed genes (DEGs) with 872 up-regulated genes, which were functionally enriched into Gene Ontol. terms pertaining to extracellular matrix (ECM) and extracellular region. KEGG enrichment for the DEGs uncovered that the activations of ECM-receptor interaction and focal adhesion pathways could be the underlying mol. mechanism implicated in the (PS)2 induced reproductive behavior impairment. This work would deliver a substantial contribution to the understanding of the ecol. safety of MePTs biocides.

Chemosphere published new progress about Behavior. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, SDS of cas: 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Matsumoto, Kyosuke; Kusaba, Shunsuke; Tanaka, Yuya; Sei, Yoshihisa; Akita, Munetaka; Aritani, Kazushi; Haga, Masa-aki; Yoshizawa, Michito published the artcile< A Peanut-Shaped Polyaromatic Capsule: Solvent-Dependent Transformation and Electronic Properties of a Non-Contacted Fullerene Dimer>, Reference of 329214-79-1, the main research area is palladium pyridylanthracene derivative capsule guest encapsulation fullerene complex preparation; crystal structure palladium pyridylanthracene derivative guest encapsulation fullerene complex; cyclic voltammetry palladium pyridylanthracene derivative guest encapsulation fullerene complex; coordination capsules; encapsulation; fullerenes; radical anions; supramolecular chemistry.

Synthesis of mol. containers capable of incorporating multiple fullerenes remains challenging. Reported here is that room-temperature mixing of metal ions with W-shaped bispyridine ligands featuring polyaromatic panels results in the quant. formation of a peanut-shaped M2L4 capsule. The capsule reversibly converts into two mols. of an ML2 double tube in response to changes in the solvent. Notably, the capsule allows the incorporation of two fullerene mols. into the connected two spherical cavities at room temperature The close proximity yet non-contact of the encapsulated C60 mols., with a separation of 6.4 Å, was revealed by x-ray crystallog. anal. The resultant, unusual fullerene dimer undergoes sequential reduction within the capsule to generate (C60.-)2, C60.-·C602-, and (C602-)2 species. Furthermore, temperature-controlled stepwise incorporation of two C60 mols. into the capsule is demonstrated.

Angewandte Chemie, International Edition published new progress about Cage compounds Role: PEP (Physical, Engineering or Chemical Process), PRP (Properties), SPN (Synthetic Preparation), PROC (Process), PREP (Preparation). 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Reference of 329214-79-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Suschitzky, H.; Chivers, G. E. published the artcile< Polyhaloaromatic compounds. XXI. Novel reagent system for the N-oxidation of weakly basic N-heteroaromatic compounds>, Safety of 2,3,4,6-Tetrachloropyridine, the main research area is pyridine oxidation pyridine oxide preparation; pyridazine oxidation pyridazine oxide preparation; pyrazine oxidation pyrazine oxide preparation; substitution nucleophilic pyridine.

By use of H2O2-H2SO4-AcOH or-CF3CO2H, pentachloro-, 2,3,4,6-tetrachloro-, 2,6-dichloro-, tetrachloro-4-nitro-, and pentabromopyridine, and tetrachloropyridazine and -pyrazine were oxidized to their N-oxides in >50% yields. 3,5-Dichloro-2,4,6-trifluoropyridine was oxidized by H2O2-polyphosphoric acid to give 3,5-dichloro-2,4-difluoro-6-hydroxypyridine 1-oxide; pentachloropyridine reacted with AcOH-H2SO4 to give 2,3,4,5-tetrachloro-6-hydroxypyridine by nucleophilic substitution.

Journal of the Chemical Society [Section] C: Organic published new progress about Oxidation. 14121-36-9 belongs to class pyridine-derivatives, and the molecular formula is C5HCl4N, Safety of 2,3,4,6-Tetrachloropyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hara, Naofumi; Uemura, Nao; Nakao, Yoshiaki published the artcile< C2-Selective silylation of pyridines by a rhodium-aluminum complex>, Safety of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine, the main research area is dehydrogenative silylation CH activation pyridine rhodium aluminum heterobimetallic catalyst; Lewis acid rhodium aluminum heterobimetallic complex dehydrogenative silylation catalyst; crystal mol structure rhodium aluminum heterobimetallic complex.

We have developed a C2-selective dehydrogenative mono-silylation of a variety of pyridines using a Rh-Al complex [(R2PCH2N-1,2-C6H4NMe-1,2-C6H4NCH2PR2)AlClRhCl(L)]n (R = Ph, iPr; n = 1, L = nbd; n = 2, L void). Both the site- and mono-selectivity are controlled via the pyridine coordination to the Lewis-acidic Al center prior to the activation of the pyridine C(2)-H bond at the proximal Rh center. A reaction mechanism is proposed based on several mechanistic studies, including the isolation of a (2-pyridyl)silylrhodium intermediate.

Chemical Communications (Cambridge, United Kingdom) published new progress about C-H bond activation. 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Safety of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem