Tag: M.W=200-250

Zhang, Rui-Qian; Liu, Zhan-Qing; Luo, Yan-Ling; Xu, Feng; Chen, Ya-Shao published the artcile< Tri-stimuli responsive carbon nanotubes covered by mesoporous silica graft copolymer multifunctional materials for intracellular drug delivery>, Application In Synthesis of 2127-03-9, the main research area is carbon silica graft copolymer multifunctional material intracellular drug delivery.

To overcome premature drug leakage and instability in drug delivery systems, we designed tri-stimuli responsive multiwalled carbon nanotubes covered by mesoporous silica graft poly(N-isopropylacrylamide-block-poly(2-(4-formylbenzoyloxy)) Et methacrylate) multifunctional materials via disulfide linkages (MWCNTs@MSN-s-s-g-PNIPAM-b-PFBEMA). The multifunctional materials could covalently bind and phys. load anticancer drug doxorubicin (DOX), and exhibited pH-, temperature- and reductant-induced multi-stimuli responsiveness, significantly enhancing drug loading capacity and improving the release dynamics of drug. The DOX-loaded multifunctional materials exhibited the optimal release behavior in cancer environments compared with in normal cells upon simultaneously triggered by these stimuli. It meant that the MWCNTs@MSN-s-s-g-PNIPAM-b-PFBEMA could serve as efficient gatekeepers to control the mesopore on-off and thus to modulate drug release. The multifunctional materials were proved to be low toxic, whereas the DOX-loaded counterparts had almost the same toxicity as free DOX to cancer cells. Therefore, the developed multifunctional materials can be used as promising drug controlled delivery platforms for cancer therapy.

Journal of Industrial and Engineering Chemistry (Amsterdam, Netherlands) published new progress about Binding energy. 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

Fang, Lei; Zhao, Zitong; Wang, Jue; Xiao, Ping; Sun, Xiangshi; Ding, Yaping; Zhang, Pengcheng; Wang, Dangge; Li, Yaping published the artcile< Light-controllable charge-reversal nanoparticles with polyinosinic-polycytidylic acid for enhancing immunotherapy of triple negative breast cancer>, SDS of cas: 2127-03-9, the main research area is charge reversal nanoparticle polyinosinic polycytidylic acid delivery cancer immunotherapy; Cancer immunotherapy; Charge-reversal; Nanoparticles; Photodynamic therapy; Polyinosinic-polycytidylic acid; ROS-responsive; Triple negative breast cancer; Tumor microenvironment.

Nucleic acid drugs are highly applicable for cancer immunotherapy with promising therapeutic effects, while targeting delivery of these drugs to disease lesions remains challenging. Cationic polymeric nanoparticles have paved the way for efficient delivery of nucleic acid drugs, and achieved stimuli-responsive disassembly in tumor microenvironment (TME). However, TME is highly heterogeneous between individuals, and most nanocarriers lack active-control over the release of loaded nucleic acid drugs, which will definitely reduce the therapeutic efficacy. Herein, we have developed a light-controllable charge-reversal nanoparticle (LCCN) with controlled release of polyinosinic-polycytidylic acid [Poly(I:C)] to treat triple neg. breast cancer (TNBC) by enhanced photodynamic immunotherapy. The nanoparticles keep suitably pos. charge for stable loading of Poly(I:C), while rapidly reverse to neg. charge after near-IR light irradiation to release Poly(I:C). LCCN-Poly(I:C) nanoparticles trigger effective phototoxicity and immunogenic cell death on 4T1 tumor cells, elevate antitumor immune responses and inhibit the growth of primary and abscopal 4T1 tumors in mice. The approach provides a promising strategy for controlled release of various nucleic acid-based immune modulators, which may enhance the efficacy of photodynamic immunotherapy against TNBC.

Acta Pharmaceutica Sinica B published new progress about Antitumor agents. 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

Heusler, Arne; Fliege, Julian; Wagener, Tobias; Glorius, Frank published the artcile< Substituted Dihydropyridine Synthesis by Dearomatization of Pyridines>, Synthetic Route of 329214-79-1, the main research area is dihydropyridine preparation regioselective; pyridine triflic anhydride dearomatization trimethylamine borane; phenyl chloroformate pyridine dearomatization trimethylamine borane; boranes; chemoselectivity; nitrogen heterocycles; reduction; synthetic methods.

The synthesis of a broad variety of N-substituted 1,4-dihydropyridines I [R = H, 3-Me, 3,5-di-Br, etc.; R1 = Tf, CO2Ph] and 1,2-dihydropyridines II [R2 = F, Cl, CF3, Ph, SPh; R3 = H, F, trimethylsilyl] by very mild and selective reduction with amine borane was reported for the first time.

Angewandte Chemie, International Edition published new progress about Dearomatization. 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Synthetic Route of 329214-79-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ebrahimi, Mahmoud; Es’haghi, Zarrin; Samadi, Fatemeh; Bamoharram, Fatemeh Farrash; Hosseini, Mohammad-Saeid published the artcile< Rational design of heteropolyacid-based nanosorbent for hollow fiber solid phase microextraction of organophosphorus residues in hair samples>, Name: 4-(Pyridin-1-ium-1-yl)butane-1-sulfonate, the main research area is organophosphorus pesticide microextraction human hair ionic liquid.

A novel heteropolyacid-based supported ionic liquid (IL) mediated sol-gel hybrid organic-inorganic is presented for effective use in hollow fiber solid phase microextraction (HF-SPME). The authors examined a Keggin-based IL that was evaluated in conjunction with sol-gel. This study shows that Keggin-based IL sol-gel generated porous morphol. pro effective extraction media. The method was developed for the extraction of the organophosphorus pesticides (OPs); diazinon, fenitrothion and malathion from human hair samples. The OPs were subsequently analyzed with HPLC and photodiode array detection (HPLC-PDA). In the basic condition (pH 10-11), the gel growth process in the presence of IL was initiated. Afterward, this sol was injected into a polypropylene hollow fiber segment for in situ-gelation process. Parameters affecting the efficiency of HF-SPME were thoroughly investigated. Linearity was observed over a range of 0.02-50,000 μg/g and 0.0001-25,000 ng/mL with detection limits between 0.0074-1.3000 μg/g and 0.00034-0.84 ng/mL for the OPs in hair and aqueous matrixes, resp. The relative recoveries in the real samples, for OPs in the storekeeper hair ranged from 86 to 95.2%.

Journal of Chromatography A published new progress about Hair. 21876-43-7 belongs to class pyridine-derivatives, and the molecular formula is C9H13NO3S, Name: 4-(Pyridin-1-ium-1-yl)butane-1-sulfonate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Sikder, Amrita; Ray, Debes; Aswal, Vinod K.; Ghosh, Suhrit published the artcile< Supramolecular Assembly of a Molecularly Engineered Protein and Polymer>, Computed Properties of 2127-03-9, the main research area is supramol assembly protein polymer; conjugation; hydrogen bonds; polymers; proteins; self-assembly.

Programmable assembly of biomols. is a fast growing research area that aims to emulate nature’s elegance in creating numerous hierarchical self-assembled structures, which are responsible for unimaginably difficult biol. functions. Protein assembly is a particularly challenging task, owing to their structural diversity, conformational heterogeneity, and high mol. weight This article reveals the ability of a supramol. structure-directing unit (SSDU) to regulate the entropically favorable supramol. assembly of a covalently conjugated protein (bovine serum albumin (BSA)) to produce well-defined protein-decorated micelles with remarkably high thermal stability, suppression of the thermal denaturation of the protein, and retention of enzymic activity. Furthermore, a SSDU-appended thermo-responsive poly(N-isopropylacrylamide) (PNIPAM) coassembles with the SSDU-BSA conjugate because, in both cases, assembly was primarily driven by specific mol. recognition between the SSDUs. However, the resulting supramol. protein-polymer conjugate exhibits distinctly different polymersome structure to that of the micellar particle produced by the protein-SSDU conjugate. In this case, the enzymic activity can be significantly suppressed above the lower critical solution temperature of supramolecularly conjugated PNIPAM, possibly due to collapse of the de-solvated polymer chains on the protein surface.

Chemistry – A European Journal published new progress about Bovine serum albumin Role: PEP (Physical, Engineering or Chemical Process), PRP (Properties), PROC (Process) (conjugates with 1,4,5,8-naphthalenetetracarboxylic diimide derivative). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Computed Properties of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Sahani, Rajkumar Lalji; Diana-Rivero, Raquel; Vernekar, Sanjeev Kumar V.; Wang, Lei; Du, Haijuan; Zhang, Huanchun; Castaner, Andres Emanuelli; Casey, Mary C.; Kirby, Karen A.; Tedbury, Philip R.; Xie, Jiashu; Sarafianos, Stefan G.; Wang, Zhengqiang published the artcile< Design, synthesis and characterization of HIV-1 CA-targeting small molecules: conformational restriction of PF74>, Computed Properties of 53636-56-9, the main research area is indolyl pyridyl amide preparation antiviral SAR cytotoxicity mol docking; imidazolyl indolyl amide preparation antiviral SAR cytotoxicity mol docking; HIV-1; PF74; capsid protein; conformational constraint; metabolic stability.

Designed and synthesized three series of PF74-like analogs featuring conformational constraints at the aniline terminus or the phenylalanine carboxamide moiety, and characterized them using a biophys. thermal shift assay (TSA), cell-based antiviral and cytotoxicity assays, and in vitro metabolic stability assays in human and mouse liver microsomes. These studies showed that the two series with the phenylalanine carboxamide moiety replaced by a pyridine or imidazole ring can provide viable hits. Subsequent SAR identified an improved analog I which effectively inhibited HIV-1 (EC50 = 0.31μM), strongly stabilized CA hexamer (ΔTm = 8.7°C), and exhibited substantially enhanced metabolic stability (t1/2 = 27 min for 15 vs. 0.7 min for PF74). Metabolic profiles from the microsomal stability assay also indicate that blocking the C5 position of the indole ring could lead to increased resistance to oxidative metabolism

Viruses published new progress about Amides Role: PAC (Pharmacological Activity), PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 53636-56-9 belongs to class pyridine-derivatives, and the molecular formula is C7H6BrNO2, Computed Properties of 53636-56-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Li, Ze; Li, Wenwei; Lu, Maolin; Bess, Julian Jr; Chao, Cara W.; Gorman, Jason; Terry, Daniel S.; Zhang, Baoshan; Zhou, Tongqing; Blanchard, Scott C.; Kwong, Peter D.; Lifson, Jeffrey D.; Mothes, Walther; Liu, Jun published the artcile< Subnanometer structures of HIV-1 envelope trimers on aldrithiol-2-inactivated virus particles>, Recommanded Product: 1,2-Di(pyridin-2-yl)disulfane, the main research area is .

Abstract: The HIV-1 envelope glycoprotein (Env) trimer, composed of gp120 and gp41 subunits, mediates viral entry into cells. Recombinant Env trimers have been studied structurally, but characterization of Env embedded in intact virus membranes has been limited to low resolution Here, we deploy cryo-electron tomog. and subtomogram averaging to determine the structures of Env trimers on aldrithiol-2 (AT-2)-inactivated virions in ligand-free, antibody-bound and CD4-bound forms at subnanometer resolution Tomog. reconstructions document mol. features consistent with high-resolution structures of engineered soluble and detergent-solubilized Env trimers. One of three conformational states previously predicted by smFRET was not observed by cryo-ET, potentially owing to AT-2 inactivation. We did observe Env trimers to open in situ in response to CD4 binding, with an outward movement of gp120-variable loops and an extension of a critical gp41 helix. Overall features of Env trimer embedded in AT-2-treated virions appear well-represented by current engineered trimers.

Nature Structural & Molecular Biology published new progress about 2127-03-9. 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

Grongsaard, Pintipa; Bulger, Paul G.; Wallace, Debra J.; Tan, Lushi; Chen, Qinghao; Dolman, Sarah J.; Nyrop, Jason; Hoerrner, R. Scott; Weisel, Mark; Arredondo, Juan; Itoh, Takahiro; Xie, Chengfu; Wen, Xianghui; Zhao, Dalian; Muzzio, Daniel J.; Bassan, Ephraim M.; Shultz, C. Scott published the artcile< Convergent, Kilogram Scale Synthesis of an Akt Kinase Inhibitor>, Synthetic Route of 1050501-88-6, the main research area is convergent synthesis AKT kinase inhibitor.

The development of a convergent, chromatog.-free synthesis of an allosteric Akt kinase inhibitor is described. The route comprised 17 total steps and was used to produce kilogram quantities of the target mol. A key early transformation, for which both batch and flow protocols were developed, was formylation of a dianion derived by deprotonation and subsequent lithium-halogen exchange from a 2-bromo-3-aminopyridine precursor. Improved reaction yield and practicality were achieved in the continuous processing mode. Further significant process developments included the safe execution of a high temperature and pressure hydrazine displacement, separation of substituted cyclobutane diastereomers by means of chemoselective ester hydrolysis, and a late-stage Suzuki fragment coupling under mild conditions.

Organic Process Research & Development published new progress about Formylation. 1050501-88-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4BrClN2, Synthetic Route of 1050501-88-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Haratipour, Pouya; Minard, Corinne; Nakhjiri, Maryam; Negahbani, Amirsoheil; Kashemirov, Boris A.; McKenna, Charles E. published the artcile< New chirally modified bisphosphonates for synthesis of individual beta,gamma-CHX-deoxynucleotide diastereomers>, Quality Control of 2127-03-9, the main research area is Mitsunobu condensation phosphonate methylmandelate ester cytosine ethylbenzylamide preparation; nucleotide ethylbenzylamine phenylglycine hydrogenolysis phosphonate protecting group nitrobenzyl; synthon deoxynucleotide polymerase kinase enzyme active site; chiral bisphosphonates; dNTP probes; polymerase mechanism.

Individual diastereomers of CXY bisphosphonate analogs of dNTPs or NTPs are useful chem. stereoprobes to investigate interactions within the chiral active site environment of enzymes such as polymerases and kinases. We previously reported synthetic access to β,γ-CHX-dGTPs (X = F or Cl) via a bisphosphonate synthon with an (R)-Me mandelate auxiliary and have extended this approach to dTTP and dATP analogs. As removal of the chiral auxiliary by (Pd/C) hydrogenolysis is incompatible with the cytosine heterocycle and also with X = Br, we have now designed bisphosphonate synthons using (R)-(+)-α-ethylbenzylamine or Me (R)-(-)-phenylglycine auxiliaries and equipped with an o-nitrobenzyl ester protecting group allowing photochem. deprotection. These new synthons have made possible the first syntheses of individual dCTP and mono-bromo-substituted dNTP β,γ-CHX diastereomers.

Phosphorus, Sulfur and Silicon and the Related Elements published new progress about Condensation reaction. 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

Inai, Makoto; Ouchi, Hitoshi; Asahina, Aya; Asakawa, Tomohiro; Hamashima, Yoshitaka; Kan, Toshiyuki published the artcile< Practical total syntheses of acromelic acids A and B>, Name: 3-Bromo-2-chloro-6-methoxypyridine, the main research area is natural product acromelic acid total regioselective enantioselective synthesis pyrrolidine; reductive amination ortho lithiation bromination dichloropyridine; nitroalkene asym conjugate addition ketoester nickel catalyst epimerization.

Practical total syntheses of acromelic acids A and B, which were scarce natural products isolated from toxic mushroom by Shirahama and Matsumoto, were accomplished in 13 (36% total yield) and 17 steps (6.9% total yield), resp., from 2,6-dichloropyridine. Beginning with regioselective transformation of sym. 2,6-dichloropyridine by either ortho-lithiation or bromination, nitroalkenes (I) (R1 = CO2Me, OMe; R2 = OMe, CO2t-Bu) were provided. Stereoselective construction of the vicinal stereocenters at the C-3, 4 positions of acromelic acids A and B was performed by a Ni-catalyzed asym. conjugate addition of α-ketoesters to the nitroalkenes. Construction of the pyrrolidine ring was accomplished in a single operation via a sequence consisting of reduction of the nitro group, intramol. condensation with the ketone, and reduction of the resulting ketimine.

Chemical & Pharmaceutical Bulletin published new progress about Amino acids Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 777931-67-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrClNO, Name: 3-Bromo-2-chloro-6-methoxypyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem