Tag: M.W=200-250

Ran, Wei; Liu, Xiaoyu; Chang, Lu; Cai, Ying; Zheng, Chao; Liu, Jia; Li, Yaping; Zhang, Pengcheng published the artcile< Self-assembling mertansine prodrug improves tolerability and efficacy of chemotherapy against metastatic triple-negative breast cancer>, Quality Control of 2127-03-9, the main research area is self assembling mertansine prodrug nanoparticle drug delivery system; Chemotherapy; Prodrug; Self-assembly; Supramolecular; Triple-negative breast cancer.

Metastatic triple-neg. breast cancer is one of the most devastating cancer types. Systemic chemotherapy is necessary, but its clin. performance is largely limited by severe side effects. Herein, we report a mertansine prodrug, which could self-assemble into spherical nanoparticles in water and readily convert into active mertansine at the presence of glutathione. The self-assembling mertansine prodrugs (SAMPDs) entered cancer cells via a caveolae-mediated pathway and exhibited potent cytotoxicity. The self-delivering SAMPDs did not cause hemolysis, and more importantly increased maximum tolerated dose (MTD) of mertansine by 8 folds via reducing free mertansine exposure in most of the major organs. SAMPDs improved intratumoral drug exposure and showed dose-dependent antitumor activity. When dosed at MTD, SAMPDs inhibited primary tumor growth and pulmonary metastasis by 80% and 95%, while mertansine dosed at MTD only reduced primary tumor growth and metastasis by <50% and 60%, resp. Our results reveal the mechanism of in vivo biotransformation of self-assembling prodrug and highlight the unique advantages of self-assembling prodrug strategy in improving the efficacy and safety of chemotherapy. Journal of Controlled Release published new progress about Antitumor agents. 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

Shahsavari, Hamid R.; Babadi Aghakhanpour, Reza; Biglari, Abbas; Niazi, Maryam; Mastrorilli, Piero; Todisco, Stefano; Gallo, Vito; Lalinde, Elena; Moreno, M. Teresa; Gimenez, Nora; Halvagar, Mohammad Reza published the artcile< C(sp2)-C(sp2) Reductive Elimination from a Diarylplatinum(II) Complex Induced by a S-S Bond Oxidative Addition at Room Temperature>, Product Details of C10H8N2S2, the main research area is arylplatinum benzothiazolethiolate pyridinethiolate preparation crystal structure; crystal structure diarylplatinum benzothiazolethiolate pyridinethiolate dinuclear platinum lantern complex; mol structure diarylplatinum benzothiazolethiolate pyridinethiolate dinuclear platinum lantern complex; dinuclear platinum lantern complex preparation crystal structure; diarylplatinum complex oxidative addition benzothiazolethiolate pyridinethiolate.

The synthesis and characterization of three six-coordinated Pt(IV) complexes [Pt(Ar)2(S[symbol omitted]N)2] (S[symbol omitted]N = Sbt, benzothiazole-2-thiolate, Ar = p-MeC6H4 (1a), C6F5 (1b); S[symbol omitted]N = Spy, 2-pyridinethiolate, Ar = p-MeC6H4 (1c)) is described. Of these, 1a undergoes, at room temperature and within 18 h, a remarkable C-C reductive elimination process between the aryl ligands to give, as the final products, the stable binuclear lantern complex [Pt2(Sbt)4] (2a) and 4,4′-dimethylbiphenyl. Differently from 1a, solutions of 1b,c are indefinetively stable up to 60° and do not undergo reductive elimination. Complexes 1a-c and 2a were characterized by IR and NMR spectroscopy, high-resolution mass spectrometry, and single-crystal x-ray crystallog. (1b,c and 2a). 1H-19F HOESY experiments on 1b demonstrated the presence of a through-space coupling between proximal F and H atoms of the mol. that are separated by six bonds but are in close spatial proximity.

Organometallics published new progress about Crystal structure. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Product Details of C10H8N2S2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jiao, Chen; Obst, Franziska; Geisler, Martin; Che, Yunjiao; Richter, Andreas; Appelhans, Dietmar; Gaitzsch, Jens; Voit, Brigitte published the artcile< Reversible Protein Capture and Release by Redox-Responsive Hydrogel in Microfluidics>, Product Details of C10H8N2S2, the main research area is protein capture redox responsive hydrogel microfluidics; disulfide bonds; hydrogels; mechanical properties; microfluidics; protein capture and release; redox-responsive; swelling behaviors.

Stimuli-responsive hydrogels have a wide range of potential applications in microfluidics, which has drawn great attention. Double crosslinked hydrogels are very well suited for this application as they offer both stability and the required responsive behavior. Here, we report the integration of poly(N-isopropylacrylamide) (PNiPAAm) hydrogel with a permanent crosslinker (N,N′-methylenebisacrylamide, BIS) and a redox responsive reversible crosslinker (N,N′-bis(acryloyl)cystamine, BAC) into a microfluidic device through photopolymerization Cleavage and re-formation of disulfide bonds introduced by BAC changed the crosslinking densities of the hydrogel dots, making them swell or shrink. Rheol. measurements allowed for selecting hydrogels that withstand long-term shear forces present in microfluidic devices under continuous flow. Once implemented, the thiol-disulfide exchange allowed the hydrogel dots to successfully capture and release the protein bovine serum albumin (BSA). BSA was labeled with rhodamine B and functionalized with 2-(2-pyridyldithio)-ethylamine (PDA) to introduce disulfide bonds. The reversible capture and release of the protein reached an efficiency of 83.6% in release rate and could be repeated over 3 cycles within the microfluidic device. These results demonstrate that our redox-responsive hydrogel dots enable the dynamic capture and release of various different functionalized (macro)mols. (e.g., proteins and drugs) and have a great potential to be integrated into a lab-on-a-chip device for detection and/or delivery.

Polymers (Basel, Switzerland) published new progress about Bovine serum albumin Role: PEP (Physical, Engineering or Chemical Process), PUR (Purification or Recovery), PROC (Process), PREP (Preparation) (rhodamine B and PDA-labeled). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Product Details of C10H8N2S2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wu, Guangyu; Liu, Xiaoman; Zhou, Pei; Xu, Zhijun; Hegazy, Mohammad; Huang, Xin; Huang, Yudong published the artcile< The construction of thiol-functionalized DNAsomes with small molecules response and protein release>, HPLC of Formula: 2127-03-9, the main research area is thiol functionalized DNAsome protein release drug delivery system; Pickering emulsion; Polymeric capsule; Self-assembly.

In this work, a poly(N-isopropylacrylamide) polymer (PNIPAAm) was prepared via the photoinduced reversible addition-fragmentation chain transfer (RAFT) polymerization using Ru(bpy)3Cl2·6H2O as photoinitiator. The design and spontaneous assembly of thiol-functionalized DNA-Thiol/PNIPAAm polymeric capsule (DNAsomes) by water-in-oil Pickering emulsion method and effective response with small mols. (Sybr green and phenanthrene) were described. The intermediate product, DNA-Thiol/PNIPAAm conjugates and DNAsomes were characterized by using 1H NMR, dynamic light scattering (DLS), SEM, TEM and UV-vis methods. The obtained results indicated that DNA-Thiol/PNIPAAm constructs assembled in a Pickering emulsion could produce DNA-based spherical DNAsomes with typically 3.3-267.7μm in diameter The DNAsomes showed a vesicle formation approx. 2μm in diameter, resulting in phenanthrene mol. intercalating with DNAsomes. The phenomenon indicated that the DNA-Thiol/PNIPAAm conjugates may have potential applications in recognition polycyclic aromatic hydrocarbon mols. The membrane of the DNAsomes could effective response toward small mols. such as Sybr green or phenanthrene, and DNAsomes has release capability of protein (BSA) under reductive agent glutathione (GSH). Our results highlight the potential of integrating aspects of supramol. and polymer chem. into the design and construction of DNA-polymeric capsule, guest mol. encapsulation, control delivery of drugs, recognition organic polycyclic aromatic hydrocarbon mols. and gene-directed capsule synthesis.

Materials Science & Engineering, C: Materials for Biological Applications published new progress about Bovine serum albumin Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, HPLC of Formula: 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hoque, Emdadul Md; Bisht, Ranjana; Unnikrishnan, Anju; Dey, Sayan; Mahamudul Hassan, Mirja Md; Guria, Saikat; Rai, Rama Nand; Sunoj, Raghavan B.; Chattopadhyay, Buddhadeb published the artcile< Iridium-Catalyzed Ligand-Controlled Remote para-Selective C-H Activation and Borylation of Twisted Aromatic Amides>, Synthetic Route of 329214-79-1, the main research area is regioselective remote para borylation CH activation twisted aromatic amide; aryl boronate preparation regioselective remote para borylation aromatic amide; potential energy surface para CH borylation twisted aromatic amide; Borylation; C−H Activation; Density Functional Calculations; Iridium Catalyst; Para Selectivity.

A method of para-selective borylation of fully twisted aromatic amides ArCONBoc2 is described, yielding boronamides 4-pinBC6HnX4-nCONBoc2 (X = alkyl, alkoxy, aryl, halo, CN). The borylation proceeded via an unprecedented substrate-ligand distortion between the twisted aromatic amides and a newly designed ligand framework, 4,5-diaza-9H-fluorene (defa) that is different from the traditionally used ligand (dtbpy) for the C-H borylation reactions. The designed ligand defa has led to the development of a new type of catalytic system that shows excellent para selectivity for a range of aromatic amides. Moreover, the designed ligand has shown excellent reactivity and selectivity for a range of heterocyclic aromatic amides. The identification of key transition states and intermediates using the DFT computations associated with the three regio-isomeric pathways revealed that the most efficient catalytic pathway with the defa ligand leads to the para borylation while in the case of bpy the borylation at the para and meta sites compete.

Angewandte Chemie, International Edition published new progress about Aromatic amides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 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

Gomes, Jose R. B.; Amaral, Luisa M. P. F.; Ribeiro da Silva, Manuel A. V. published the artcile< Gas-phase thermochemistry of chloropyridines>, Electric Literature of 14121-36-9, the main research area is chloropyridine formation enthalpy metal cation affinity.

The gas-phase standard molar enthalpy of formation of 2,3,5-trichloropyridine was derived from the enthalpies of combustion of the crystalline solid measured by rotating-bomb calorimetry and its enthalpy of sublimation obtained by Calvet microcalorimetry at T = 298.15 K. The standard enthalpies of formation for this compound and for the other chloro-substituted pyridines were determined by DFT calculations The exptl. enthalpy of formation of 2,3,5-trichloropyridine is (65.8 ± 2.3) kJ mol-1, in excellent agreement with the B3LYP/6-311+G(2d,2p)//B3LYP/6-31G(d) value. The affinity of pyridine to some metal cations was also calculated at the same DFT level of theory and compared with exptl. data.

Chemical Physics Letters published new progress about Binding energy (of pyridine- and chloropyridine-cation complexes). 14121-36-9 belongs to class pyridine-derivatives, and the molecular formula is C5HCl4N, Electric Literature of 14121-36-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Nitelet, Antoine; Thevenet, Damien; Schiavi, Bruno; Hardouin, Christophe; Fournier, Jean; Tamion, Rodolphe; Pannecoucke, Xavier; Jubault, Philippe; Poisson, Thomas published the artcile< Copper-Photocatalyzed Borylation of Organic Halides under Batch and Continuous-Flow Conditions>, Formula: C11H16BNO2, the main research area is copper photocatalyzed borylation aryl heteroaryl vinyl alkyl halide; aryl vinyl alkyl boronic acid ester preparation electrochem; borylation; continuous flow; copper; photocatalysis; visible light.

The Cu-photocatalyzed borylation of aryl, heteroaryl, vinyl and alkyl halides (I and Br) is reported. The reaction proceeded using a new heteroleptic Cu complex under irradiation with blue LEDs, giving the corresponding boronic-acid esters in good to excellent yields. The reaction was extended to continuous-flow conditions to allow an easy scale-up. The mechanism of the reaction was studied and a mechanism based on a reductive quenching (Cu(I)/Cu(I)*/Cu(0)) was suggested.

Chemistry – A European Journal published new progress about Boronic acids, esters Role: SPN (Synthetic Preparation), PREP (Preparation). 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Formula: C11H16BNO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Cheng, Yin-Jia; Qin, Si-Yong; Ma, Yi-Han; Chen, Xiao-Sui; Zhang, Ai-Qing; Zhang, Xian-Zheng published the artcile< Super-pH-Sensitive Mesoporous Silica Nanoparticle-Based Drug Delivery System for Effective Combination Cancer Therapy>, Product Details of C10H8N2S2, the main research area is peptide doxorubicin silica nanoparticle tumor antitumor; charge-reversal; combinational tumor therapy; mesoporous silica nanoparticles; multifunctional peptide; redox-sensitive drug release.

A multifunctional nanoplatform based on mesoporous silica nanoparticles (MSNs) was developed for combinational tumor therapy. Doxorubicin (DOX) was chosen as an antitumor drug and loaded into mesopores of MSNs via phys. absorption. Then, a tumor-targeted fusion peptide conjugated with 2,3-dimethylmaleic anhydride (DTCPP) and a therapeutic peptide conjugated with 2,3-dimethylmaleic anhydride (DTPP) were introduced to the surface of MSNs as super-pH-sensitive nanovalves through disulfide linkages. The BSA adsorption assay confirmed the charge-reversal property of MSN-ss-DTPP&DTCPP nanoparticles at slightly acidic condition (pH 6.8) and superior stability in physiol. environment (pH 7.4). According to the drug release research, both glutathione (GSH) and acidic condition are required for the accelerated drug release from DOX@MSN-ss-DTPP&DTCPP nanoparticles. Moreover, in vitro studies demonstrated the significantly reinforced tumor cellular uptake efficiency and mitochondrial disruption ability of DOX@MSN-ss-DTPP&DTCPP nanoparticles in tumor environment, in which DOX@MSN-ss-DTPP&DTCPP nanoparticles exhibited the preferred cytotoxicity toward αvβ3-pos. human cervical carcinoma (HeLa) cells. We believe that the multifunctional dual-stimuli-sensitive MSN could provide an effective strategy for combinational tumor therapy.

ACS Biomaterials Science & Engineering published new progress about Antitumor agents. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Product Details of C10H8N2S2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Li, Xuefu; Ru, Shaoguo; Tian, Hua; Zhang, Suqiu; Lin, Zhenxian; Gao, Ming; Wang, Jun published the artcile< Combined exposure to environmentally relevant copper and 2,2-dithiobis-pyridine induces significant reproductive toxicity in male guppy (Poecilia reticulata)>, Application of C10H8N2S2, the main research area is Poecilia reproductive toxicity dithiobis pyridine copper risk assessment; (PS)(2); Co-exposure; Cu; Ecological safety; Guppy (Poecilia reticulata); Impaired reproduction.

Metal pyrithiones (MePTs), the most widely used biocides in antifouling paints (AFs) coated on the hulls, are usually used in combination with Cu-containing substances. In the aquatic environment, 2,2-dithiobis-pyridine ((PS)2), the main degradation product of MePTs, and Cu usually coexist. However, their combined impacts on aquatic organisms are unclear. This study exposed male guppy (Poecilia reticulata) to an environmentally realistic concentration of Cu (10μg/L) alone or Cu (10μg/L) combined with 20, 200, and 2000 ng/L (PS)2 to explore their combined reproductive toxicity. The results showed that co-exposure to Cu and (PS)2 increased Cu accumulation in the fish body in a dose-dependent manner and induced obvious spermatozoon apoptosis and necrosis, which was mediated by the peroxidation and caspase activation. Compared to Cu alone, co-exposure to Cu and 200, 2000 ng/L (PS)2 significantly decreased the testosterone level and collapsed spermatogenesis, and depressed male sexual interest and mating behavior were observed in three co-exposure groups. Moreover, co-exposure to Cu and (PS)2 increased the disturbance on cyp19a and cyp19b transcription and suppressed the “”display”” reproductive behavior. Eventually, co-exposure to Cu and (PS)2 caused male reproductive failure. Therefore, the concurrence of Cu and (PS)2 induced significant reproductive toxicity in male guppies and would threaten the sustainability of fish populations. Considering the extensive usage of MePTs products in the AFs, their ecol. risk warrants more evaluation.

Science of the Total Environment published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (cyp19a). 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Application of C10H8N2S2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Croisy-Delcey, Martine; Bisagni, Emile published the artcile< Aza analogs of lucanthone: synthesis and antitumor and bactericidal properties>, Product Details of C9H9Cl2NO2, the main research area is aza analog lucanthone; antitumor lucanthone aza analog; bactericide lucanthone aza analog.

Aza analogs of lucanthone (e.g., I; X = S, NH) were synthesized for evaluation as antitumor drugs. None of the compounds had significant cytotoxic effects on either Friend-tumor or L1210 leukemia cells. However, I (X = NH) had noticeable antibiotic properties.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, Product Details of C9H9Cl2NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem