Month: October 2022

Sisco, Edward; Barnes, Korry L. published the artcile< Design, Synthesis, and Biological Evaluation of Novel 1,3-Oxazole Sulfonamides as Tubulin Polymerization Inhibitors>, Application In Synthesis of 29027-20-1, the main research area is oxazolyl sulfonamide preparation antitumor SAR tubulin polymerization inhibitor; cyclopropyl oxazolyl benzenesulfonyl chloride amine coupling reaction.

A series of novel 1,3-oxazole sulfonamides I (R = 4-FC6H4NH2, -CH2CH2SO2Me, 1-Naph, etc; R’ = H, Me)were constructed and screened for their potential to inhibit cancer cell growth. These compounds were evaluated against the full NCI-60 human tumor cell lines, with the majority exhibiting promising overall growth inhibitory properties. They displayed high specificity within the panel of leukemia cell lines vs. all other lines tested. When examined in the dose-response assay, GI50 values fell within the low micromolar to nanomolar ranges. 1,3-Oxazole sulfonamide I (R = 4-Cl-3-CF3C6H3NH2, R’ = H) displayed the best average growth inhibition, whereas the 2-chloro-5-methylphenyl and 1-naphthyl substituents on the sulfonamide nitrogen proved to be the most potent leukemia inhibitors with mean GI50 values of 48.8 and 44.7 nM, resp. In vitro tubulin polymerization experiments revealed that this class of compounds effectively binds to tubulin and induces the depolymerization of microtubules within cells.

ACS Medicinal Chemistry Letters published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 29027-20-1 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H8ClN, Application In Synthesis of 29027-20-1.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Liu, Wentao; Huang, Wei; Lin, Qian; Tsai, Mei-Hsuan; Zhang, Rui; Fan, Lijun; Scott, Jack D.; Liu, Guansai; Wan, Jinqiao published the artcile< Development of DNA-compatible hydroxycarbonylation reactions using chloroform as a source of carbon monoxide>, Recommanded Product: 4-Chloro-3-methoxybenzoic acid, the main research area is DNA encoded hydroxycarbonylation aryl halide chloroform; Chloroform; DNA compatible reaction; DNA-encoded library; Hydroxycarbonylation; Palladium catalysis.

A robust palladium-catalyzed hydroxycarbonylation of aryl halides on DNA has been developed. Instead of Mo(CO)6 as a source of carbon monoxide as previously described in the literature, chloroform was used as a surrogate in this report for the purpose of avoiding to use a large excess of molybdenum reagent which is not totally soluble in aqueous reaction mixtures

Bioorganic & Medicinal Chemistry published new progress about Aromatic carboxylic acids Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 85740-98-3 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO3, Recommanded Product: 4-Chloro-3-methoxybenzoic acid.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Yu, Hao; Wang, Zhenhua; Wu, Ri; Chen, Xiangfeng; Chan, T.-W. Dominic published the artcile< Water-dispersible pH/thermo dual-responsive microporous polymeric microspheres as adsorbent for dispersive solid-phase extraction of fluoroquinolones from environmental water samples and food samples>, Category: chlorides-buliding-blocks, the main research area is polymeric microsphere liquid chromatog mass spectrometry; dispersive solid phase extraction water dispersibility; Environmental samples; Hydrophilic–hydrophobic transition; Liquid chromatography–mass spectrometry; Polymeric microspheres; Water dispersibility; d-SPE.

Multifunctional polymeric microspheres were prepared using hyper-crosslinking chem. combined with surface-initiated atom transfer radical polymerization The synthesized microspheres exhibited good water dispersibility, a high surface area, and pH/thermo dual-responsiveness. Fluoroquinolones (FQs), which contains a hydrophilic piperazine ring and hydrophobic fluorine atoms, were used as target analytes to assess the performance of the microspheres as a sorbent for dispersive solid-phase extraction (d-SPE). The d-SPE exptl. parameters, including extraction time, amount of microspheres, extraction temperature, and sample solution pH, as well as the desorption conditions, were systematically studied. Coupled with LC-MS/MS, an anal. method for anal. of trace-level FQs in water samples was developed and validated. Under optimal conditions, linearity with correlation coefficients (r) of >0.99 was achieved in the concentration range of 0.02-10 μg L-1. The limits of detection and quantification for the selected FQs were 5.0-6.7 and 12-20 ng L-1, resp. High recovery values (93.1%-97.2%), a high enrichment factor (∼180), and good precision (RSD < 8%, n = 6) were obtained for FQ determination in spiked purified water samples. It was proposed that hydrophilic-hydrophobic transition induced by stretching and shrinking of polymer chains under different pH and temperature conditions offered good control of the surface wettability and altered the extraction behavior. The developed method was validated and was successfully applied to the anal. of FQs in environmental water samples, meat and milk samples. These results demonstrated that the water-dispersible polymeric microspheres have good potential for use in separation and extraction techniques. Journal of Chromatography A published new progress about Adsorbents. 1592-20-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H9Cl, Category: chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Gimenez, Rodrigo E.; Serrano, Mariana P.; Alvarez, Rosa Maria S.; Martino, Debora M.; Borsarelli, Claudio D. published the artcile< Fabrication and Characterization of Hollow Microcapsules from Polyelectrolytes Bearing Thymine Pendant Groups for Ultraviolet-B (UVB)-Induced Crosslinking>, Electric Literature of 1592-20-7, the main research area is polyelectrolyte microcapsule thymine UV crosslinking; hollow microcapsules; layer-by-layer method; photo-crosslinking; polyelectrolytes; thymine.

DNA – bioinspired polyelectrolytes poly[vinylbenzylthymine (VBT)-4-vinylbenzyltriethylammonium chloride (VBA)] and poly[vinylbenzylthymine (VBT)-4-vinylphenylsufonate (VPS)] were used for the preparation of hollow microcapsules (HMC) using the layer-by-layer method and CaCO3 microspheres as removable molds. Stable aqueous suspensions of spherical-shaped HMCs with a shell composed of six layers of VBA-based polyelectrolytes were obtained, of approx. (7.0 ± 1.5) μm diameter and a shell thickness of 1 μm. UV-B irradiation of the HMC suspensions induces an efficient crosslinking between adjacent polyelectrolyte chains through the formation of thymine photodimers, such as the cyclobutane pyrimidine dimer (CPD) and the (6-4) pyrimidine-pyrimidone photoproduct (6-4PP). This process resulted in a reduction of the average interstitial mesh size of the HMC shells, modulating their permeability properties and increasing the mech. stability of the HMC without a noticeable modification of size and shape. Thus, the DNA-bioinspired polyelectrolytes are promising materials for the preparation of UVB-responsive HMCs.

ChemPlusChem published new progress about Double-layer capacitance. 1592-20-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H9Cl, Electric Literature of 1592-20-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Smart, Daniel J.; Helbling, Fabian R.; Verardo, Maelle; Huber, Alizee; McHugh, Damian; Vanscheeuwijck, Patrick published the artcile< Development of an integrated assay in human TK6 cells to permit comprehensive genotoxicity analysis in vitro>, Product Details of C7H17Cl2N2O3P, the main research area is TK6 cell line genotoxin genotoxicity single integrated assay; Chromosome damage; Genotoxicity assessment; Mode-of-action; Mutation.

In vitro genetic toxicol. assays are used to assess the genotoxic potential of chems. or mixtures They measure chromosome damage (e.g., micronucleus [MN] formation) or gene mutation, and different combinations of data generated from such assays are evaluated in concert in order to identify genotoxic hazards. Mode-of-action (MoA) information is also fundamental to understanding any apparent genotoxic response. In view of the importance of these types of data for full characterization of genotoxic potential, we leveraged relevant endpoints already established in the human TK6 cell line to develop a single integrated assay that measures MN formation, gene mutation (at the thymidine kinase locus), and MoA (DNA damage response biomarkers). Several prototypical direct-acting genotoxins (Me methanesulfonate, mitomycin C, and 4-nitroquinoline 1-oxide), pro-genotoxins (benzo[a]pyrene and cyclophosphamide monohydrate), and one non-DNA reactive genotoxin (vinblastine sulfate) were assessed in the approach and found to elicit genotoxic profiles that were generally consistent with their MoA. In contrast, the non-genotoxic agents D-mannitol and (2-chloroethyl) trimethyl-ammonium chloride induced negligible effects on all endpoints up to a top concentration of 10 mM. Sodium diclofenac, presumed to be non-genotoxic, provoked an induction in the phosphoserine10-H3-pos. cell population within a small window of concentrations (0.157-0.314 mM), as well as increases in γH2AX, nuclear p53, and MN at higher concentrations, although it had no effect on the mutation frequency endpoint. G2M cell cycle arrest was also largely observed in cells that exhibited genotoxicity in the in vitro MN assay. The TK6 cell-based integrated assay represents an in vitro approach that permits comprehensive genotoxicity anal. in a human-relevant test system. Moreover, its vis-a-vis nature may facilitate further comprehension of the range of effects that can manifest in human cells in response to DNA-damaging agents.

Mutation Research, Genetic Toxicology and Environmental Mutagenesis published new progress about Biomarkers. 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Product Details of C7H17Cl2N2O3P.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Wang, Zian; Yao, Jingwen; Zhan, Lisi; Gong, Shaolong; Ma, Dongge; Yang, Chuluo published the artcile< Purine-based thermally activated delayed fluorescence emitters for efficient organic light-emitting diodes>, SDS of cas: 2382-10-7, the main research area is purine derivative thermally activated delayed fluorescence organic LED; diode light emitting organic purine derivative thermal delayed fluorescence; electroluminescent device organic purine derivative thermally activated delayed fluorescence.

Two thermally-activated delayed fluorescence (TADF) emitters (1PXZP and 2PXZP) based on a novel biol. base acceptor of 9-methylpurine and commonly used donor of phenoxazine (PXZ) were synthesized and characterized. Both target compounds possess nearly orthogonal configurations to reduce singlet-triplet splitting energy (ΔEST) for remarkable TADF character. The 2 emitters show good luminescence quantum yields (PLQYs), and the organic LEDs employing 1PXZP and 2PXZP as emitters display good performance with maximum external quantum efficiencies of 10.6 and 13.8%, resp. The efficiencies of 1PXZP based device show nearly no roll-off at 100 cd m-2 luminance due to the short delayed lifetime (τd) of 3.2μs. This work manifests that the biol. base is a promising acceptor for designing TADF materials.

Dyes and Pigments published new progress about Cyclic voltammetry. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, SDS of cas: 2382-10-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Liao, Ke; Wu, Fengjin; Chen, Jiean; Huang, Yong published the artcile< Catalytic cleavage and functionalization of bulky and inert Csp3-Csp3 bonds via a relayed proton-coupled electron transfer strategy>, COA of Formula: C6H4Cl2N4, the main research area is alc radicalophile acridinium tetrafluoroborate regioselective photochem bond cleavage functionalization.

The direct, photoredox cleavage of hindered Csp3-Csp3 bonds of alcs. under neutral conditions was described. A relayed proton-coupled electron transfer (PCET) strategy was employed that overcame the previous requirement of a Bronsted base. Heavily branched alcs. with a high oxidation potential (Eox1/2 > +2 V vs. SCE) were cleaved and functionalized with remarkable efficiency and versatility. A simple, non-substituted Ph group can promote a relayed PCET process to deliver primary, secondary, and tertiary alkyl radicals under neutral conditions.

Cell Reports Physical Science published new progress about Alcohols Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, COA of Formula: C6H4Cl2N4.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Morris, Joel; Wishka, Donn G.; Fang, Yue published the artcile< A cyclodehydration route to 2-aminochromones>, Safety of Methyl 4-chloro-2-hydroxybenzoate, the main research area is salicylacetamide preparation cyclodehydration; cyclocondensation salicylacetamide; aminochromone; salicylate reaction amide enolate.

Cyclodehydration of salicylacetamides I with triflic anhydride efficiently provided the corresponding 2-aminochromone II (R1 = H, 6-, 7-, 8-MeO, 6-Br, 7-Cl, 7-, 8-Me; NR2 = NMe2, 4-morpholino) in 59-79% yield. The use of polyphosphoric ester (PPE) for this process was somewhat less effective. However, the deacylated derivative of compound II (R1 = AcNH, NR2 = 4-morpholino) was prepared in only 10% yield with triflic anhydride as reagent, whereas PPE as reagent afforded the expected compound II in 44% yield. Compounds I were prepared by reaction of substituted Me salicylates with an amide enolate.

Synthetic Communications published new progress about Cyclocondensation reaction. 22717-55-1 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO3, Safety of Methyl 4-chloro-2-hydroxybenzoate.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Zhou, Fei; Zhang, Yanhua; Xu, Xiufang; Luo, Jingfeng; Yang, Fang; Wang, Linbo; Xie, Shuduo; Sun, Jihong; Yang, Xiaoming published the artcile< Establishment and characterization of three stable Basal/HER2-positive breast cancer cell lines derived from Chinese breast carcinoma with identical missense mutations in the DNA-binding domain of TP53>, Reference of 6055-19-2, the main research area is TP53 mutation HER2 prognosis breast cancer population; Basal/HER2-positive; Breast cancer cell lines; Epithelial cell; Invasive ductal breast carcinoma; STR.

Background: Basal/human epidermal growth factor receptor (HER)2-pos. (HER2+) breast cancer is resistant to monoclonal antibody (herceptin) treatment. There are currently only three basal/HER2+ breast cancer cell lines available, but they are not from Chinese populations. Methods: Three immortalized cell lines (ZJU-0327, ZJU-0725, and ZJU-1127) were established from invasive ductal breast carcinoma tissue of two patients treated by surgical resection at our center. The cell lines were characterized in terms of histol., therapeutic response, and biomarker expression. Their tumorigenic potential was evaluated in an athymic nude (BALB/C nu) mouse xenograft model. Cell authentication testing by the techniques of short tandem repeat. Results: ZJU-0327, ZJU-0725, and ZJU-1127 cell lines were maintained for more than 110 passages in vitro. The cells grew as monolayers; showed typical epithelial morphol. and ultrastructure; were polyploid; had doubling times of 18, 57.5, and 18 h, resp.; had a near-tetraploid (ZJU-0327 and ZJU-1127) or aneuploid (ZJU-0725) karyotype with structural aberrations and tumor protein 53 mutation; insensitive to chemotherapeutic drugs and/or radiation; show high invasiveness and tumorigenicity in mice; and had no mycoplasma contamination. The cell lines were basal/HER2+, expressed cluster of differentiation, and were associated with poor prognosis. Cell authentication testing by the American Type Culture Collection confirmed the human origin of the cell lines, which did not match those in existing databases. Conclusions: The three novel basal/HER2+ breast cancer cell lines recapitulating the malignant characteristics of the parent tumor’s, and can be useful for clarifying the mol. pathogenesis of basal/HER2+ breast cancer.

Cancer Cell International published new progress about Animal gene Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study) (HER2). 6055-19-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H17Cl2N2O3P, Reference of 6055-19-2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Jun, Joonhong; Baek, Jihyun; Yang, Songyi; Moon, Hyungwoo; Kim, Hyejin; Cho, Hyunwook; Hah, Jung-Mi published the artcile< Discovery of a Potent and Selective JNK3 Inhibitor with Neuroprotective Effect Against Amyloid β-Induced Neurotoxicity in Primary Rat Neurons>, Quality Control of 27841-33-4, the main research area is amyloid beta neurotoxicity Jun terminal kinase inhibitor neuroprotective effect; Alzheimer’s disease (AD); JNK3; SAR; benzimidazole; neurodegenerative diseases; neuroprotection.

As members of the MAPK family, c-Jun-N-terminal kinases (JNKs) regulate the biol. processes of apoptosis. In particular, the isoform JNK3 is expressed explicitly in the brain at high levels and is involved in the pathogenesis of neurodegenerative diseases such as Alzheimer′s disease (AD) and Parkinson′s disease (PD). In this study, we prepared a series of five 6-dihydroxy-1H-benzo[d]imidazoles as JNK3 inhibitors and found them have potential as neuroprotective agents. Following a previous lead scaffold, benzimidazole moiety was modified with various aryl groups and hydroxylation, and the resulting compounds exhibited JNK3 inhibitory activity with improved potency and selectivity. Out of 37 analogs synthesized, (S)-cyclopropyl(3-((4-(2-(2,3-dihydrobenzo[b][1,4]dioxin -6-yl)-5,6-dihydroxy-1H-benzo[d]imidazol-1-yl)pyrimidin-2-yl)amino) piperidin-1-yl)methanone (35b) demonstrated the highest JNK3 inhibition (IC50 = 9.7 nM), as well as neuroprotective effects against Aβ-induced neuronal cell death. As a protein kinase inhibitor, it also showed excellent selectivity over other protein kinases including isoforms JNK1 (>1000 fold) and JNK2 (-10 fold).

International Journal of Molecular Sciences published new progress about Cell viability. 27841-33-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H12N2O2, Quality Control of 27841-33-4.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics