Tag: M.W=200-250

Estabrook, Daniel A.; Day, Rachael A.; Sletten, Ellen M. published the artcile< Redox-Responsive Gene Delivery from Perfluorocarbon Nanoemulsions through Cleavable Poly(2-oxazoline) Surfactants>, Safety of 1,2-Di(pyridin-2-yl)disulfane, the main research area is polyoxazoline surfactant perfluorocarbon nanoemulsion redox responsive gene delivery; emulsions; gene delivery; interfacial chemistry; poly(2-oxazoline); stimuli-responsive carriers.

The clin. utility of emulsions as delivery vehicles is hindered by a dependence on passive release. Stimuli-responsive emulsions overcome this limitation but rely on external triggers or are composed of nanoparticle-stabilized droplets that preclude sizes necessary for biomedical applications. Here, we employ cleavable poly(2-oxazoline) diblock copolymer surfactants to form perfluorocarbon (PFC) nanoemulsions that release cargo upon exposure to glutathione. These surfactants allow for the first example of redox-responsive nanoemulsions in cellulo. A noncovalent fluorous tagging strategy is leveraged to solubilize a GFP plasmid inside the PFC nanoemulsions, whereupon protein expression is achieved selectively when employing a stimuli-responsive surfactant. This work contributes a methodol. for non-viral gene delivery and represents a general approach to nanoemulsions that respond to endogenous stimuli.

Angewandte Chemie, International Edition published new progress about Drug delivery systems. 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

Hao, Shu-Yi; Qi, Zhi-Yuan; Wang, Shuai; Wang, Xing-Rong; Chen, Shi-Wu published the artcile< Synthesis and bioevaluation of N-(3,4,5-trimethoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-amines as tubulin polymerization inhibitors with anti-angiogenic effects>, Related Products of 777931-67-6, the main research area is pyridopyrazole trimethoxyaniline palladium acetate catalyst haloalkane Buchwald Hartwig coupling; trimethoxyphenyl pyrazolo pyridinamine preparation antitumor cytotoxicity SAR; Aniogenesis; Antitumor; Inhibitors; Pyrazolo[3,4-b]pyridine; Tubulin polymerization.

A new series of N-(3,4,5-trimethoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-amine derivatives I [R1 = H, Me, cyclopentyl; R2 = Me, Et, Pr, etc.] as tubulin polymerization inhibitors were synthesized, and evaluated for the anti-proliferative activities. A structure-activity relationship study revealed that the free amino moiety of 1H-pyrazolo[3,4-b]pyridin-3-amine played an essential role in the anti-proliferative activities. Especially, compound I [R1 = H; R2 = methyl] displayed the strongest anti-proliferation against MCF-7 cells with IC50 value of 0.067 ± 0.003μM, and high selectivity over the normal human embryonic lung WI-38 cells with IC50 value of 23.41 ± 1.53μM. Further mechanistic studies revealed that I [R1 = H; R2 = methyl] showed strong anti-tubulin polymerization activity, changed the morphol. of tubulin, and arrested the cell cycle at the G2/M transition in MCF-7 cells. Mol. docking anal. suggested that I [R1 = H; R2 = methyl] well occupied the colchicine-binding pocket of tubulin. Addnl., I [R1 = H; R2 = methyl] demonstrated anti-angiogenic activities with blocking the migration, invasion and tube formation, disrupting the newly formed tube, and regulating both MMP-9 and TIMP-1 in HUVEC cells. In summary,results highlight that compound I [R1 = H; R2 = methyl] was a potential antitumor compound that was worthy of further development.

Bioorganic & Medicinal Chemistry published new progress about Antiangiogenic agents. 777931-67-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrClNO, Related Products of 777931-67-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mittelbach, Martin published the artcile< An easy and convenient synthesis of 6-methyl-4(1H)-pyridone-3-carboxylic acid>, Reference of 86129-63-7, the main research area is nicotinic acid dihydro oxo methyl.

The title acid (I) was prepared from a nicotinic acid derivative Et 2,4-dichloro-6-methylnicotinate was treated with Na and R1OH (R1 = Me, Et), the alkoxy analog products II were subjected to reductive dechlorination, and the products were hydrolyzed by HCl to give I.

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

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Huang, Zhiyong; Wang, Dan; Long, Cheng-Yu; Li, Shen-Huan; Wang, Xue-Qiang; Tan, Weihong published the artcile< Regulating the Anticancer Efficacy of Sgc8-Combretastatin A4 Conjugates: A Case of Recognizing the Significance of Linker Chemistry for the Design of Aptamer-Based Targeted Drug Delivery Strategies>, Recommanded Product: 1,2-Di(pyridin-2-yl)disulfane, the main research area is aptamer targeted drug delivery anticancer efficacy cytotoxicity cell viability.

The unique merits of aptamers, including specificity, high binding affinity, easy cell internalization, and rapid tissue accumulation abilities, have led aptamer-drug conjugates to evolve into one of the most attractive strategies for targeted drug delivery purposes. Nevertheless, the critical role of linkers in regulating anticancer efficacy of these conjugates, especially those engineered by automated modular synthesis techniques, has been rarely explored. In this work, we utilized Sgc8c aptamer and combretastatin A4 to develop three conjugates with either a phosphodiester bond linker, a disulfide bond linker, or a carbamate linker to study their payload release mechanisms and the influence on anticancer efficacy. These investigations allowed us to identify the unique activation pathway of the phosphodiester bond linker that is activated by both nucleophilic attack of glutathione and degradation caused by phosphodiesterase, which is highly associated with the higher cytotoxicity of the conjugate. Importantly, the understanding of the chem. of phosphodiester bond linker activation allowed us to further design another XQ-2d-CA4 conjugate that can induce pancreatic cancer cells apoptosis in a more efficient manner.

Journal of the American Chemical Society published new progress about Antitumor agents. 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

Tkachuk, Viktor M.; Lukianov, Oleh O.; Vovk, Mykhailo V.; Gillaizeau, Isabelle; Sukach, Volodymyr A. published the artcile< Chan-Evans-Lam N1-(het)arylation and N1-alkenylation of 4-fluoroalkylpyrimidin-2(1H)-ones>, Related Products of 329214-79-1, the main research area is substituted pyrimidone preparation; fluoroalkylpyrimidinone boronic acid arylation alkenylation copper catalyst; alkenylboronic acid pinacol ester fluoroalkylpyrimidinone arylation alkenylation copper catalyst; Chan–Evans–Lam reaction; C–N cross-coupling; boronic acids; fluoroalkyl group; pyrimidin-2(1Н)-ones.

The Chan-Evans-Lam reaction of 1-unsubstituted 4-fluoroalkylpyrimidin-2(1H)-ones with arylboronic acids was reported as a facile synthetic route to hitherto unavailable N1-(het)aryl and N1-alkenyl derivatives of the corresponding pyrimidines I [R = CH=CH2, Ph, 3-thienyl, etc.; R1 = CHF2, CF3, C2F5, CClF2; R2 = H, Br, CO2Me]. An efficient C-N bond-forming process was also observed by using boronic acid pinacol esters as coupling partners in the presence of Cu(II) acetate and boric acid. The 4-fluoroalkyl group on the pyrimidine ring significantly assists in the formation of the target N1-substituted products, in contrast to the 4-Me and 4-unsubstituted substrates which did not undergo N1-arylation under similar reaction conditions.

Beilstein Journal of Organic Chemistry published new progress about Alkenylation. 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Related Products of 329214-79-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Zhi; Lin, Yi-An; Kim, Soo-Young; Su, Lilly; Liu, Jinhuan; Kannan, Rangaramanujam M.; Kannan, Sujatha published the artcile< Systemic dendrimer-drug nanomedicines for long-term treatment of mild-moderate cerebral palsy in a rabbit model>, Quality Control of 2127-03-9, the main research area is dendrimer antioxidant anti inflammatory agent drug release; Cerebral palsy; Microglia; NAC; Neurobehavior; Neuroinflammation; PAMAM dendrimers.

Background: Neuroinflammation mediated by microglia plays a central role in the pathogenesis of perinatal/neonatal brain injury, including cerebral palsy (CP). Therapeutics mitigating neuroinflammation potentially provide an effective strategy to slow the disease progression and rescue normal brain development. Building on our prior results which showed that a generation-4 hydroxyl poly(amidoamine) (PAMAM) dendrimer could deliver drugs specifically to activated glia from systemic circulation, we evaluated the sustained efficacy of a generation-6 (G6) hydroxyl-terminated PAMAM dendrimer that showed a longer blood circulation time and increased brain accumulation. N-acetyl-L-cysteine (NAC), an antioxidant and anti-inflammatory agent that has high plasma protein binding properties and poor brain penetration, was conjugated to G6-PAMAM dendrimer-NAC (G6D-NAC). The efficacy of microglia-targeted G6D-NAC conjugate was evaluated in a clin. relevant rabbit model of CP, with a mild/moderate CP phenotype to provide a longer survival of untreated CP kits, enabling the assessment of sustained efficacy over 15 days of life. Methods: G6D-NAC was conjugated and characterized. Cytotoxicity and anti-inflammatory assays were performed in BV-2 microglial cells. The efficacy of G6D-NAC was evaluated in a rabbit model of CP. CP kits were randomly divided into 5 groups on postnatal day 1 (PND1) and received an i.v. injection of a single dose of PBS, or G6D-NAC (2 or 5 mg/kg), or NAC (2 or 5 mg/kg). Neurobehavioral tests, microglia morphol., and neuroinflammation were evaluated at postnatal day 5 (PND5) and day 15 (PND15). Results: A single dose of systemic ‘long circulating’ G6D-NAC showed a significant penetration across the impaired blood-brain-barrier (BBB), delivered NAC specifically to activated microglia, and significantly reduced microglia-mediated neuroinflammation in both the cortex and cerebellum white matter areas. Moreover, G6D-NAC treatment significantly improved neonatal rabbit survival rate and rescued motor function to nearly healthy control levels at least up to 15 days after birth (PND15), while CP kits treated with free NAC died before PND9. Conclusions: Targeted delivery of therapeutics to activated microglia in neonatal brain injury can ameliorate pro-inflammatory microglial responses to injury, promote survival rate, and improve neurol. outcomes that can be sustained for a long period. Appropriate manipulation of activated microglia enabled by G6D-NAC can impact the injury significantly beyond inflammation.

Journal of Neuroinflammation published new progress about Animal gene, TGFB1 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Quality Control of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Blumbergs, Peter; Ash, Arthur B.; Daniher, F. A.; Stevens, Calvin Lee; Michel, H. O.; Hackley, B. E. Jr.; Epstein, J. published the artcile< Alkylating agents containing a quaternary nitrogen group>, Category: pyridine-derivatives, the main research area is alkylating sulfonates; sulfonates alkylating; pyridinium sulfonates.

A series of 18 new, water-soluble alkylating agents was synthesized. The structures contain an alkylsulfonate group as the alkylating function and a quaternary ammonium salt group attached to a hydrocarbon backbone. Some pyridinium sulfonates perchlorates were also prepared

Journal of Organic Chemistry published new progress about 21876-43-7. 21876-43-7 belongs to class pyridine-derivatives, and the molecular formula is C9H13NO3S, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Bellini, Michela; Riva, Benedetta; Tinelli, Veronica; Rizzuto, Maria Antonietta; Salvioni, Lucia; Colombo, Miriam; Mingozzi, Francesca; Visioli, Alberto; Marongiu, Laura; Frascotti, Gianni; Christodoulou, Michael S.; Passarella, Daniele; Prosperi, Davide; Fiandra, Luisa published the artcile< Engineered Ferritin Nanoparticles for the Bioluminescence Tracking of Nanodrug Delivery in Cancer>, Synthetic Route of 2127-03-9, the main research area is ferritin nanoparticle bioluminescence imaging cancer; apoferritin nanoparticles; luciferase/luciferin; nanomedicine; self-immolative linkers; tumor targeting.

The identification of a highly sensitive method to check the delivery of administered nanodrugs into the tumor cells is a crucial step of preclin. studies aimed to develop new nanoformulated cures, since it allows the real therapeutic potential of these devices to be forecast. In the present work, the ability of an H-ferritin (HFn) nanocage, already investigated as a powerful tool for cancer therapy thanks to its ability to actively interact with the transferrin receptor 1, to act as an efficient probe for the monitoring of nanodrug delivery to tumors is demonstrated. The final formulation is a bioluminescent nanoparticle, where the luciferin probe is conjugated on nanoparticle surface by means of a disulfide containing linker (Luc-linker@HFn) which is subjected to glutathione-induced cyclization in tumor cell cytoplasm. The prolonged imaging of luciferase+ tumor models, demonstrated by an in vitro and an in vivo approach, associated with the prolonged release of luciferin into cancer cells by disulfide bridge reduction, clearly indicates the high efficiency of Luc-linker@HFn for drug delivery to the tumor tissues.

Small published new progress about Apoferritins Role: NAN (Nanomaterial), THU (Therapeutic Use), BIOL (Biological Study), USES (Uses). 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

Cui, Yahan; Deng, Rong; Li, Xiangshuai; Wang, Xinghuo; Jia, Qiong; Bertrand, Emilie; Meguellati, Kamel; Yang, Ying-Wei published the artcile< Temperature-sensitive polypeptide brushes-coated mesoporous silica nanoparticles for dual-responsive drug release>, Application of C10H8N2S2, the main research area is temperature polypeptide mesoporous silica nanoparticle.

A biopolymer-inorganic hybrid system (MSN@PBLGF) is designed and fabricated from mesoporous silica nanoparticles (MSNs) and folic acid (FA)-terminated temperature-sensitive synthetic polypeptide, i.e., poly(γ-benzyl-L-glutamate) (PBLG) derivative, through a thiol-disulfide exchange reaction, where MSNs with high drug loading capacity serve as drug nanocarriers and the biocompatible PBLG biopolymer brushes installed on MSN surface through disulfide bonds endow the system with tumor-specific recognition ability and GSH/temperature dual-stimuli responsiveness. Controlled drug release experiments indicate that DOX can be tightly hosted in the system with limited premature release, but efficiently released in response to an increased concentration of GSH and/or an elevated temperature Intracellular experiments demonstrate that the DOX-loaded MSN@PBLGF nanohybrid shows outstanding cellular uptake and cell-growth inhibition effects on human lung cancer cell line A549 in comparison with healthy human cells such as hepatocyte cells LO2.

Chinese Chemical Letters 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

Pal, Sunirmal; Sommerfeldt, Andreas; Davidsen, Maiken B.; Hinge, Mogens; Pedersen, Steen U.; Daasbjerg, Kim published the artcile< Synthesis and Closed-Loop Recycling of Self-Immolative Poly(dithiothreitol)>, Category: pyridine-derivatives, the main research area is recycling self immolative polydithiothreitol.

Self-immolative polymers (SIPs) are promising members of the emerging class of recyclable polymers with the ability to end-to-end depolymerize to their monomers. Unfortunately, SIPs are often synthesized by cumbersome procedures at low temperatures in protected atm. In this study, a SIP with a novel poly(disulfide) backbone is introduced, using DL-dithiothreitol (DTT) as the monomer. Remarkably, poly(DTT) can be produced by solid-state polymerization in a robust and easily scalable process by mech. mixing DTT with 2,2′-dithiodipyridine as the end-capping agent. The new polymer possesses good thermal and chem. stabilities, but once its depolymerization is triggered, this proceeds smoothly within minutes to afford cyclic DTT because of a favorable intramol. back-biting thiol-disulfide exchange reaction in the polymer backbone. As a proof of concept, the cyclic DTT waste was recovered, reduced to DTT monomer, and repolymd. in a closed-loop approach.

Macromolecules (Washington, DC, United States) published new progress about Chemical stability. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem