Zhou, Sen’s team published research in Journal of Organic Chemistry in 2021-05-07 | 2127-03-9

Journal of Organic Chemistry published new progress about One-pot synthesis. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Name: 1,2-Di(pyridin-2-yl)disulfane.

Zhou, Sen; Hou, Xiaoya; Yang, Kai; Guo, Minjie; Zhao, Wentao; Tang, Xiangyang; Wang, Guangwei published the artcile< Direct Synthesis of N-Difluoromethyl-2-pyridones from Pyridines>, Name: 1,2-Di(pyridin-2-yl)disulfane, the main research area is difluoromethylpyridone difluoromethylquinolinone preparation.

A novel method for the synthesis of N-difluoromethyl-2-pyridones was described. This protocol enables the synthesis of N-difluoromethyl-2-pyridones from readily available pyridines using mild reaction conditions that are compatible with a wide range of functional groups. The preliminary mechanistic study revealed that N-difluoromethylpyridinium salts were the key intermediates to complete this conversion.

Journal of Organic Chemistry published new progress about One-pot synthesis. 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

Darwish, Shaban’s team published research in European Journal of Medicinal Chemistry in 2019-01-01 | 2127-03-9

European Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Safety of 1,2-Di(pyridin-2-yl)disulfane.

Darwish, Shaban; Sadeghiani, Neda; Fong, Shirley; Mozaffari, Saghar; Hamidi, Parinaz; Withana, Thimanthi; Yang, Sun; Tiwari, Rakesh Kumar; Parang, Keykavous published the artcile< Synthesis and antiproliferative activities of doxorubicin thiol conjugates and doxorubicin-SS-cyclic peptide>, Safety of 1,2-Di(pyridin-2-yl)disulfane, the main research area is human embryonic kidney ovarian fibrosarcoma leukemia; cyclopeptide preparation antitumor doxorubicin fluorescence cellular uptake chemotherapy antiproliferative; Anticancer; Cardiotoxicity; Cellular uptake; Cyclic peptide; Disulfide; Doxorubicin; Thiol.

Myocardial toxicity and drug resistance caused by drug efflux are major limitations of doxorubicin (Dox)-based chemotherapy. Dox structure modification could be used to develop conjugates with an improved biol. profile, such as antiproliferative activity and higher cellular retention. Thus, Dox thiol conjugates, Dox thiol (Dox-SH), thiol-reactive Dox-SS-pyridine (SS = disulfide), and a Dox-SS-cell-penetrating cyclic peptide, Dox-SS-[C(WR)4K], were synthesized. Dox was reacted with Traut’s reagent to generate Dox-SH. Cytotoxicity of the compounds was examined in human embryonic kidney (HEK-293), human ovarian cancer (SKOV-3), human fibrosarcoma (HT-1080), and human leukemia (CCRF-CEM) cells. These data indicate that Dox-SH, Dox-SS-Pyr, and Dox-SS-[C(WR)4K] have the potential to be further examined as Dox alternatives and anticancer agents.

European Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 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

Mori, Kisho’s team published research in Angewandte Chemie, International Edition in 2019 | 2127-03-9

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.

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

Dan, Krishna’s team published research in Nature Nanotechnology in 2019-03-31 | 2127-03-9

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.

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

Zheng, Meng’s team published research in Angewandte Chemie, International Edition in 2019 | 2127-03-9

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.

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

Chakroun, Rami W’s team published research in ACS Nano in 2019-07-23 | 2127-03-9

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.

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

Kassem, Salma’s team published research in Chemical Science in 2021 | 2127-03-9

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.

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

Leer, Katharina’s team published research in Nanoscale in 2021 | 2127-03-9

Nanoscale published new progress about Cell viability. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Synthetic Route of 2127-03-9.

Leer, Katharina; Cinar, Gizem; Solomun, Jana I.; Martin, Liam; Nischang, Ivo; Traeger, Anja published the artcile< Core-crosslinked, temperature- and pH-responsive micelles: design, physicochemical characterization, and gene delivery application>, Synthetic Route of 2127-03-9, the main research area is block copolymer micelles temperature pH gene delivery cytotoxicity.

Stimuli-responsive block copolymer micelles can provide tailored properties for the efficient delivery of genetic material. In particular, temperature- and pH-responsive materials are of interest, since their physicochem. properties can be easily tailored to meet the requirements for successful gene delivery. Within this study, a stimuli-responsive micelle system for gene delivery was designed based on a diblock copolymer consisting of poly(N,N-diethylacrylamide) (PDEAm) as a temperature-responsive segment combined with poly(aminoethyl acrylamide) (PAEAm) as a pH-responsive, cationic segment. Upon temperature increase, the PDEAm block becomes hydrophobic due to its lower critical solution temperature (LCST), leading to micelle formation. Furthermore, the monomer 2-(pyridin-2-yldisulfanyl)ethyl acrylate (PDSAc) was incorporated into the temperature-responsive PDEAm building block enabling disulfide crosslinking of the formed micelle core to stabilize its structure regardless of temperature and dilution The cloud points of the PDEAm block and the diblock copolymer were investigated by turbidimetry and fluorescence spectroscopy. The temperature-dependent formation of micelles was analyzed by dynamic light scattering (DLS) and elucidated in detail by an anal. ultracentrifuge (AUC), which provided detailed insights into the solution dynamics between polymers and assembled micelles as a function of temperature Finally, the micelles were investigated for their applicability as gene delivery vectors by evaluation of cytotoxicity, pDNA binding, and transfection efficiency using HEK293T cells. The investigations showed that core-crosslinking resulted in a 13-fold increase in observed transfection efficiency. Our study presents a comprehensive investigation from polymer synthesis to an in-depth physicochem. characterization and biol. application of a crosslinked micelle system including stimuli-responsive behavior.

Nanoscale published new progress about Cell viability. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Synthetic Route of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Saidalimu, Ibrayim’s team published research in Organic Chemistry Frontiers in 2019 | 2127-03-9

Organic Chemistry Frontiers published new progress about Aromatic compounds, disulfides Role: RCT (Reactant), RACT (Reactant or Reagent). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Synthetic Route of 2127-03-9.

Saidalimu, Ibrayim; Liang, Yumeng; Niina, Kiyoteru; Tanagawa, Kazuhiro; Saito, Norimichi; Shibata, Norio published the artcile< Synthesis of aryl and heteroaryl tetrafluoro-λ6-sulfanyl chlorides from diaryl disulfides using trichloroisocyanuric acid and potassium fluoride>, Synthetic Route of 2127-03-9, the main research area is aryl heteroaryl tetrafluoro sulfanyl chloride preparation; diaryl disulfide trichloroisocyanuric acid potassium fluoride oxidative chlorotetrafluorination.

A catalyst-free method for the synthesis of aryl and heteroaryl tetrafluoro-λ6-sulfanyl chlorides (Ar-SF4Cl) by using trichloroisocyanuric acid and potassium fluoride in acetonitrile was presented. The method has wide substrate generality and proceeded well with high yields even in the absence of acid catalysts. The preparation of meta- and para-SF4Cl-substituted pyridines using TCCA was achieved for the first time.

Organic Chemistry Frontiers published new progress about Aromatic compounds, disulfides Role: RCT (Reactant), RACT (Reactant or Reagent). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Synthetic Route of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kufka, Rainer’s team published research in Beilstein Journal of Organic Chemistry in 2019 | 2127-03-9

Beilstein Journal of Organic Chemistry published new progress about Antitumor agents. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Safety of 1,2-Di(pyridin-2-yl)disulfane.

Kufka, Rainer; Rennert, Robert; Kaludjerovic, Goran N.; Weber, Lutz; Richter, Wolfgang; Wessjohann, Ludger A. published the artcile< Synthesis of a tubugi-1-toxin conjugate by a modulizable disulfide linker system with a neuropeptide Y analogue showing selectivity for hY1R-overexpressing tumor cells>, Safety of 1,2-Di(pyridin-2-yl)disulfane, the main research area is breast colon prostate cancer tubugi 1 toxin neuropeptide Y; PDC; Ugi reaction; drug targeting; neuropeptide Y; peptide–drug conjugate; targeted tumor therapy; tubugi; tubulysin A.

Tubugi-1 is a small cytotoxic peptide with picomolar cytotoxicity. To improve its cancer cell targeting, it was conjugated using a universal, modular disulfide derivative This allowed conjugation to a neuropeptide-Y (NPY)-inspired peptide [K4(C-βA-),F7,L17,P34]-hNPY, acting as NPY Y1 receptor (hY1R)-targeting peptide, to form a tubugi-1-SS-NPY disulfide-linked conjugate. The cytotoxic impacts of the novel tubugi-1-NPY peptide-toxin conjugate, as well as of free tubugi-1, and tubugi-1 bearing the thiol spacer (liberated from tubugi-1-NPY conjugate), and native tubulysin A as reference were investigated by in vitro cell viability and proliferation screenings. The tumor cell lines HT-29, Colo320 (both colon cancer), PC-3 (prostate cancer), and in conjunction with RT-qPCR analyses of the hY1R expression, the cell lines SK-N-MC (Ewing′s sarcoma), MDA-MB-468, MDA-MB-231 (both breast cancer) and 184B5 (normal breast; chem. transformed) were investigated. As hoped, the toxicity of tubugi-1 was masked, with IC50 values decreased by ca. 1,000-fold compared to the free toxin. Due to intracellular linker cleavage, the cytotoxic potency of the liberated tubugi-1 that, however, still bears the thiol spacer (tubugi-1-SH) was restored and up to 10-fold higher compared to the entire peptide-toxin conjugate. The conjugate shows toxic selectivity to tumor cell lines overexpressing the hY1R receptor subtype like, e.g., the hard to treat triple-neg. breast cancer MDAMB- 468 cells.

Beilstein Journal of Organic Chemistry published new progress about Antitumor agents. 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