Tag: M.W=200-250

Mori, Kisho; Hirase, Mitsuhiro; Morishige, Takahiro; Takano, Eri; Sunayama, Hirobumi; Kitayama, Yukiya; Inubushi, Sachiko; Sasaki, Ryohei; Yashiro, Masakazu; Takeuchi, Toshifumi published the artcile< A Pretreatment-Free, Polymer-Based Platform Prepared by Molecular Imprinting and Post-Imprinting Modifications for Sensing Intact Exosomes>, Recommanded Product: 1,2-Di(pyridin-2-yl)disulfane, the main research area is exosome detection fluorescence polymer sensing platform antibody cancer; exosomes; fluorescence; membrane proteins; molecular imprinting; post-imprinting modifications.

Exosomes are small (30-100 nm) membrane vesicles that serve as regulatory agents for intercellular communication in cancers. Currently, exosomes are detected by immuno-based assays with appropriate pretreatments like ultracentrifugation and are time consuming (>12 h). We present a novel pretreatment-free fluorescence-based sensing platform for intact exosomes, wherein exchangeable antibodies and fluorescent reporter mols. were aligned inside exosome-binding cavities. Such antibody-containing fluorescent reporter-grafted nanocavities were prepared on a substrate by well-designed mol. imprinting and post-imprinting modifications to introduce antibodies and fluorescent reporter mols. only inside the binding nanocavities, enabling sufficiently high sensitivity to detect intact exosomes without pretreatment. The effectiveness of the system was demonstrated by using it to discriminate between normal exosomes and those originating from prostate cancer and analyze exosomes in tear drops.

Angewandte Chemie, International Edition published new progress about Antibodies and Immunoglobulins Role: ARU (Analytical Role, Unclassified), TEM (Technical or Engineered Material Use), ANST (Analytical Study), USES (Uses) (anti-CD9). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Recommanded Product: 1,2-Di(pyridin-2-yl)disulfane.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hou, Shaohua; Yang, Xiping; Yang, Yuejing; Tong, Yu; Chen, Quanwei; Wan, Boheng; Wei, Ran; Lu, Tao; Chen, Yadong; Hu, Qinghua published the artcile< Design, synthesis and biological evaluation of 1H-indazole derivatives as novel ASK1 inhibitors>, COA of Formula: C11H16BNO2, the main research area is aryl indazole preparation ASK inhibition mol docking SAR; 1H-indazole derivatives; ASK1 inhibitor; Inflammatory bowel disease.

A series of novel ASK1 inhibitors, e.g., I and II with 1H-indazole scaffold were designed, synthesized and evaluated for their ASK1 kinase activity and AP1-HEK293 cell inhibitory effect. Systematic structure-activity relationship (SAR) efforts led to the discovery of promising compound II, which showed excellent in vitro ASK1 kinase activity and potent inhibitory effects on ASK1 in AP1-HEK293 cells. In a tumor necrosis factor-α (TNF-α)-induced HT-29 intestinal epithelial cell model, compound II exhibited a significantly protective effect on cell viability comparable to that of GS-4997; moreover, compound II exhibited no obvious cytotoxicity against HT-29 cells at concentrations up to 25μM. Mechanistic research demonstrated that compound II suppressed phosphorylation in the ASK1-p38/JNK signaling pathway in HT-29 cells and regulated the expression levels of apoptosis-related proteins. Altogether, these results showed that compound II may serve as a potential candidate compound for the treatment of inflammatory bowel disease (IBD).

European Journal of Medicinal Chemistry published new progress about Amides Role: PAC (Pharmacological Activity), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, COA of Formula: C11H16BNO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Dunn, A. D. published the artcile< The addition of hydroxylamine to derivatives of halopyridine carboxylic acids>, Recommanded Product: Methyl 3-bromo-2-pyridinecarboxylate, the main research area is halopyridinecarboxylate hydroxylamine addition; pyridinecarboxylate halo hydroxylamine addition; halopyridinenitrile hydroxylamine cyclization; isoxazolopyridine.

Cyanopyridines I (R = Cl, R1 = cyano, R2 = H; R = cyano, R1 = Cl, R2 = H; R = H, R1 = cyano, R2 = Cl) reacted with a MeOH solution of NH2OH and MeONa to give isoxazolopyridines. Thus, I (R = Cl, R1 = cyano, R2 = H) gave isoxazolopyridine II. However, I (R = H, R1 = Cl, R2 = cyano) reacted with the same reagent to give I (R, R1, same, R2 = CONH2), and I (R = H, R1 = Br, R2 = cyano) gave I [R, R1, same, R2 = C(:NOH)NH2]. No bicyclic products were formed . Esters I (R = Cl, R1 = CO2Me, R2 = H) reacted with the same reagent to give the hydroxamic acids I (R, R2, same, R1 = CONHOH). Similarly esters I (R = CO2Me, R1 = Br, R2 = H; R= H, R1 = Br, R2 = CO2Me) also gave the corresponding hydroxamic acids.

Zeitschrift fuer Chemie published new progress about Cyclocondensation reaction. 53636-56-9 belongs to class pyridine-derivatives, and the molecular formula is C7H6BrNO2, Recommanded Product: Methyl 3-bromo-2-pyridinecarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Keller, P. A. published the artcile< Product class 2: pyridinones and related systems>, Category: pyridine-derivatives, the main research area is review pyridinone preparation; pyridinethione preparation review; pyridineselenone preparation review; pyridinetellurone preparation review.

A review of methods to prepare pyridinones and related systems is presented. Synthetic methods include cyclization, aromatization, ring transformation, and substituent modification. The parent pyridinones are generally stable and are easily handled under standard laboratory conditions. The corresponding pyridinethiones are generally more reactive but have the advantage of generally requiring only standard laboratory equipment for their handling. The pyridineselenones are more reactive and the pyridinetellurones have not been comprehensively studied and characterized due to their reactivity and associated difficulty in production

Science of Synthesis published new progress about Aromatization. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Miller, Susanne L.; Chotana, Ghayoor A.; Fritz, Jonathan A.; Chattopadhyay, Buddhadeb; Maleczka, Robert E. Jr.; Smith, Milton R. III published the artcile< C-H Borylation Catalysts that Distinguish Between Similarly Sized Substituents Like Fluorine and Hydrogen>, Product Details of C7H9BrN2, the main research area is aromatic compound carbon hydrogen bond activation borylation iridium catalyst; borane heteroaryl derivative preparation.

By modifying ligand steric and electronic profiles it is possible to C-H borylate ortho or meta to substituents in aromatic and heteroaromatic compounds, where steric differences between accessible C-H sites are small. Dramatic effects on selectivities between reactions using B2pin2 or 4,4,5,5-tetramethyl-1,3,2-dioxaborolane (HBpin) are described for the 1st time. Judicious ligand and borane combinations give highly regioselective C-H borylations on substrates where typical borylation protocols afford poor selectivities.

Organic Letters published new progress about Boranes Role: SPN (Synthetic Preparation), PREP (Preparation) ((hetero)aromatic). 396092-82-3 belongs to class pyridine-derivatives, and the molecular formula is C7H9BrN2, Product Details of C7H9BrN2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kassem, Salma; Lee, Alan T. L.; Leigh, David A.; Markevicius, Augustinas; Tetlow, Daniel J.; Toriumi, Naoyuki published the artcile< Site-to-site peptide transport on a molecular platform using a small-molecule robotic arm>, Application of C10H8N2S2, the main research area is small mol robotic arm peptide transport.

Peptides attached to a cysteine hydrazide ‘transporter module’ are transported selectively in either direction between two chem. similar sites on a mol. platform, enabled by the discovery of new operating methods for a mol. transporter that functions through ratcheting. Substrate repositioning is achieved using a small-mol. robotic arm controlled by a protonation-mediated rotary switch and attachment/release dynamic covalent chem. A polar solvent mixtures were found to favor Z to E isomerization of the doubly-protonated switch, transporting cargo in one direction (arbitrarily defined as ‘forward’) in up to 85% yield, while polar solvent mixtures were unexpectedly found to favor E to Z isomerization enabling transport in the reverse (‘backward’) direction in >98% yield. Transport of the substrates proceeded in a matter of hours (compared to 6 days even for simple cargoes with the original system) without the peptides at any time dissociating from the machine nor exchanging with others in the bulk. Under the new operating conditions, key intermediates of the switch are sufficiently stabilized within the macrocycle formed between switch, arm, substrate and platform that they can be identified and structurally characterized by 1H NMR. The size of the peptide cargo has no significant effect on the rate or efficiency of transport in either direction. The new operating conditions allow detailed phys. organic chem. of the ratcheted transport mechanism to be uncovered, improve efficiency, and enable the transport of more complex cargoes than was previously possible.

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

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Chakroun, Rami W.; Wang, Feihu; Lin, Ran; Wang, Yin; Su, Hao; Pompa, Danielle; Cui, Honggang published the artcile< Fine-Tuning the Linear Release Rate of Paclitaxel-Bearing Supramolecular Filament Hydrogels through Molecular Engineering>, Name: 1,2-Di(pyridin-2-yl)disulfane, the main research area is paclitaxel prodrug peptide hydrogel; chemotherapy; controlled release; drug delivery; hydrogels; molecular assembly; prodrug.

One key design feature in the development of any local drug delivery system is the controlled release of therapeutic agents over a certain period of time. In this context, we report the characteristic feature of a supramol. filament hydrogel system that enables a linear and sustainable drug release over the period of several months. Through covalent linkage with a short peptide sequence, we are able to convert an anticancer drug, paclitaxel (PTX), to a class of prodrug hydrogelators with varying critical gelation concentrations These self-assembling PTX prodrugs associate into filamentous nanostructures in aqueous conditions and consequently percolate into a supramol. filament network in the presence of appropriate counterions. The intriguing linear drug release profile is rooted in the supramol. nature of the self-assembling filaments which maintain a constant monomer concentration at the gelation conditions. We found that mol. engineering of the prodrug design, such as varying the number of oppositely charged amino acids or through the incorporation of hydrophobic segments, allows for the fine-tuning of the PTX linear release rate. In cell studies, these PTX prodrugs can exert effective cytotoxicity against glioblastoma cell lines and also primary brain cancer cells derived from patients and show enhanced tumor penetration in a cancer spheroid model. We believe this drug-bearing hydrogel platform offers an exciting opportunity for the local treatment of human diseases.

ACS Nano published new progress about Amphiphiles. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Name: 1,2-Di(pyridin-2-yl)disulfane.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zheng, Meng; Jiang, Tong; Yang, Wen; Zou, Yan; Wu, Haigang; Liu, Xiuhua; Zhu, Fengping; Qian, Rongjun; Ling, Daishun; McDonald, Kerrie; Shi, Jinjun; Shi, Bingyang published the artcile< The siRNAsome: A Cation-Free and Versatile Nanostructure for siRNA and Drug Co-delivery>, Application of C10H8N2S2, the main research area is siRNAsome nanostructure siRNA drug codelivery; co-delivery; nanostructures; siRNA; synergistic therapy; vesicles.

Nanoparticles show great potential for drug delivery. However, suitable nanostructures capable of loading a range of drugs together with the co-delivery of siRNAs, which avoid the problem of cation-associated cytotoxicity, are lacking. Herein, we report an small interfering RNA (siRNA)-based vesicle (siRNAsome), which consists of a hydrophilic siRNA shell, a thermal- and intracellular-reduction-sensitive hydrophobic median layer, and an empty aqueous interior that meets this need. The siRNAsome can serve as a versatile nanostructure to load drug agents with divergent chem. properties, therapeutic proteins as well as co-delivering immobilized siRNAs without transfection agents. Importantly, the inherent thermal/reduction-responsiveness enables controlled drug loading and release. When siRNAsomes are loaded with the hydrophilic drug doxorubicin hydrochloride and anti-P-glycoprotein siRNA, synergistic therapeutic activity is achieved in multidrug resistant cancer cells and a tumor model.

Angewandte Chemie, International Edition published new progress about Antitumor agents. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Application of C10H8N2S2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Dan, Krishna; Veetil, Aneesh T.; Chakraborty, Kasturi; Krishnan, Yamuna published the artcile< DNA nanodevices map enzymatic activity in organelles>, Safety of 1,2-Di(pyridin-2-yl)disulfane, the main research area is DNA nanodevice endosomal fluorescent imaging.

Cellular reporters of enzyme activity are based on either fluorescent proteins or small mols. Such reporters provide information corresponding to wherever inside cells the enzyme is maximally active and preclude minor populations present in subcellular compartments. Here the authors describe a chem. imaging strategy to selectively interrogate minor, subcellular pools of enzymic activity. This new technol. confines the detection chem. to a designated organelle, enabling imaging of enzymic cleavage exclusively within the organelle. The authors have thus quant. mapped disulfide reduction exclusively in endosomes in Caenorhabditis elegans and identified that exchange is mediated by minor populations of the enzymes PDI-3 and TRX-1 resident in endosomes. Impeding intraendosomal disulfide reduction by knocking down TRX-1 protects nematodes from infection by Corynebacterium diphtheriae, revealing the importance of this minor pool of endosomal TRX-1. TRX-1 also mediates endosomal disulfide reduction in human cells. A range of enzymic cleavage reactions in organelles are amenable to anal. by this new reporter strategy.

Nature Nanotechnology published new progress about Caenorhabditis elegans. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Safety of 1,2-Di(pyridin-2-yl)disulfane.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Sun, Suqun; He, Min; Dai, Yuanwei; Li, Xin; Liu, Zhijun; Yao, Li published the artcile< Catalytic acetalization: an efficient strategy for high-value utilization of biodiesel-derived glycerol>, Formula: C9H13NO3S, the main research area is biodiesel derived glycerol acetalization ester sulfatefunctionalized ionic liquid catalyst.

In this study, an efficient process for high value utilization of biodiesel-derived glycerol was proposed via a simple reaction of acetalization catalyzed by novel catalysts of ester sulfatefunctionalized ionic liquids (ILs). The relationship between the IL structure and its catalytic activity was investigated. The effects of reaction conditions, and the substrate adaptability, were also carefully studied. The results demonstrate that ester sulfate-functionalized IL shows excellent catalytic activity on the acetalization of glycerol with aldehyde (ketone).Under the optimized condition, 87% glycerol conversion was obtained with 99% acetal selectivity when glycerol was condensed with cyclohexanone. In particular, 29% of product consists of six-membered compound, an important fine chem. and an excellent precursor in organic chem., because of the significant steric-hindrance effect of IL catalyst. Furthermore, the IL catalyst shows good recyclability where insignificant activity loss was exhibited even after six runs.

Catalysts published new progress about Acetalization. 21876-43-7 belongs to class pyridine-derivatives, and the molecular formula is C9H13NO3S, Formula: C9H13NO3S.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem