Month: December 2022

Valsalakumari, Remya published the artcileMechanism of cellular uptake and cytotoxicity of paclitaxel loaded lipid nanocapsules in breast cancer cells, Recommanded Product: 4-(5-(4-Methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzenesulfonamide, the publication is International Journal of Pharmaceutics (Amsterdam, Netherlands) (2021), 120217, database is CAplus and MEDLINE.

Lipid nanocapsules (LNCs) have proven their efficacy in delivering different drugs to various cancers, but no studies have yet described their uptake mechanisms, paclitaxel (PTX) delivery or resulting cytotoxicity towards breast cancer cells. Herein, we report results concerning cellular uptake of LNCs and cytotoxicity studies of PTX-loaded LNCs (LNCs-PTX) on the three breast cancer cell lines MCF-7, MDA-MB-231 and MDA-MB-468. LNCs-PTX of sizes 50 ± 2 nm, 90 ± 3 nm and 120 ± 4 nm were developed by the phase inversion method. Fluorescence microscopy and flow cytometry were used to observe the uptake of fluorescently labeled LNCs and cellular uptake of LNCs-PTX was measured using HPLC analyses of cell samples. These studies revealed a higher uptake of LNCs-PTX in MDA-MB-468 cells than in the other two cell lines. Moreover, free PTX and LNCs-PTX exhibited a similar pattern of toxicity towards each cell line, but MDA-MB-468 cells appeared to be more sensitive than the other two cell lines, as evaluated by the MTT cytotoxicity assay and a cell proliferation assay based upon [3H]thymidine incorporation. Studies with inhibitors of endocytosis indicate that the cellular uptake is mainly via the Cdc42/GRAF-dependent endocytosis as well as by macropinocytosis, whereas dynamin-dependent processes are not required. Furthermore, our results indicate that endocytosis of LNCs-PTX is important for the toxic effect on cells. Western blot anal. revealed that LNCs-PTX induce cytotoxicity by means of apoptosis in all the three cell lines. Altogether, the results demonstrate that LNCs-PTX exploit different mechanisms of endocytosis in a cell-type dependent manner, and subsequently induce apoptotic cell death in the breast cancer cells here studied. The article also describes biodistribution studies following i.v. injection of fluorescently labeled LNCs in mice.

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about 71203-35-5. 71203-35-5 belongs to pyrazoles-derivatives, auxiliary class GPCR/G Protein,Ras, name is 4-(5-(4-Methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C12H9N3O4, Recommanded Product: 4-(5-(4-Methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzenesulfonamide.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Tong, Chao-Lai published the artcileNucleophilic and Radical Heptafluoroisopropoxylation with Redox-Active Reagents, SDS of cas: 1289010-13-4, the publication is Angewandte Chemie, International Edition (2021), 60(42), 22915-22924, database is CAplus and MEDLINE.

The practical and efficient heptafluoroisopropoxylation reactions through the invention of a series of redox-active N-OCF(CF₃)₂ reagents e.g., I were described. These reagents were readily prepared from the oxidative heptafluoroisopropylation of hydroxylamines e.g., II with AgCF(CF₃)₂. The substitutions on the nitrogen atom significantly affected the properties and reactivities of N-OCF(CF₃)₂ reagents. Accordingly, two types of N-OCF(CF₃)₂ reagents including I and III were used as OCF(CF₃)₂ anion and radical precursors, resp. This protocol enables the direct heptafluoroisopropoxylation of a range of substrates, delivering the corresponding products in moderate to excellent yields.

Angewandte Chemie, International Edition published new progress about 1289010-13-4. 1289010-13-4 belongs to pyrazoles-derivatives, auxiliary class Pyrazoles, name is 4,6-Dichloro-2-(3-methyl-1H-pyrazol-1-yl)pyrimidine, and the molecular formula is C11H14O2, SDS of cas: 1289010-13-4.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Yan, Xingchen published the artcileProteasome inhibition and cytostatic effects on human cancer cells by pyrazolone-enamines: a combined crystallographic, structural and computational study, Application In Synthesis of 4551-69-3, the publication is New Journal of Chemistry (2015), 39(3), 2168-2180, database is CAplus.

Nine compounds were designed and synthesized by the condensation reaction of the carbonyl in 4-benzoyl-3-methyl-1-phenyl-2-pyrazolin-5-one (HPMBP) with the amino groups in 5-aminoisophthalic acid, 4,4′-diaminodiphenylmethane, 4-aminophenylacetic acid, 4-aminobenzamide, 2-amino-4-methylphenol, 5-amino-2-methylphenol, 2-aminophenol, 3-aminophenol and 4-aminophenol. They were then characterized by IR, ¹H NMR, elemental anal., and x-ray crystallog., which suggested that all of them exist as the pyrazolone-enamine forms in the solid state and in a DMSO solution through tautomeric reactions. The nine compounds were evaluated for their ability to inhibit the proliferation of human liver cancer HepG2 cells. Compounds 4-[(Z)-(2-Hydroxy-5-methylphenylamino)phenylmethylene]-3-methyl-1-phenyl-2-pyrazolin-5-one (5), 4-[(Z)-(3-Hydroxy-4-methylphenylamino)phenylmethylene]-3-methyl-1-phenyl-2-pyrazolin-5-one (6), 4-[(Z)-(2-Hydroxyphenylamino)phenylmethylene]-3-methyl-1-phenyl-2-pyrazolin-5-one (7) and 4-[(Z)-(3-Hydroxyphenylamino)phenylmethylene]-3-methyl-1-phenyl-2-pyrazolin-5-one (8) demonstrated a strong inhibitory effect on the proliferation of HepG2 cells. The nine compounds can also inhibit the activity of the human cancer cellular 20S proteasome. Further studies on compound (6) as the representative indicate that it can cause the accumulation of ubiquitinated proteins and the proteasome target proteins Bax and p27, and exhibit a cytostatic effect in HepG2 cells in a concentration-dependent and time-dependent manner. The four potential tautomers of compound (6) were optimized and their single point energies were calculated by the d. functional theory (DFT) B3LYP method based on the polarized continuum model (PCM) in water to identify the most likely tautomer existing in cancer cells. Based on the optimized structure of the most stable tautomer in water, the Wiberg bond orders, mol. electrostatic potential (MEP) maps and frontier MO were calculated As compounds (5), (6), (7) and (8) have hydroxyl in the ortho-position or meta-position, the authors’ study can provide some information to study their anticancer mechanism and the substitution effect of different functional groups.

New Journal of Chemistry published new progress about 4551-69-3. 4551-69-3 belongs to pyrazoles-derivatives, auxiliary class Benzenes, name is 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, and the molecular formula is C19H15NO3, Application In Synthesis of 4551-69-3.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Wu, Gengxin published the artcileAsymmetric Organocatalysis Combined with Palladium Catalysis: Synergistic Effect on Enantioselective Mannich/α-Allylation Sequential Reactions of Pyrazolones in Constructing Vicinal Quaternary Stereocenters, Product Details of C10H9ClN2O, the publication is Organic Letters (2019), 21(19), 7708-7712, database is CAplus and MEDLINE.

In this letter, an efficient one-pot asym. sequential reaction is achieved by organo/transition metal relay catalysis in constructing two consecutive C-C bonds, which involves enantioselective amino squaramide catalytic Mannich-type addition of pyrazolones to isatin-derived ketimines and a subsequent palladium catalyzed diastereoselective allylic alkylation of pyrazolones with allylic acetates. An array of novel pyrazolone-aminooxindole-propylene structural motifs are obtained in a high level of yield and with excellent enantio- and diastereoselectivity (up to 95% yield, >20:1 dr, >99% ee). This methodol. features the formation of vicinal quaternary carbon-stereocenters, and the second all-carbon tetrasubstituted stereogenic center is induced by joint action of the achiral palladium catalysis and the chiral environment generated from the Mannich step. Moreover, the usefulness of this methodol. is highlighted by converting the allylic product into the carbonyl compound

Organic Letters published new progress about 14580-22-4. 14580-22-4 belongs to pyrazoles-derivatives, auxiliary class Organic Pigment, name is 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, and the molecular formula is C15H14Cl2S2, Product Details of C10H9ClN2O.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Hou, Zhong-Wei published the artcileElectrophotocatalytic C-H Azolation of Arenes, HPLC of Formula: 930-36-9, the publication is ChemElectroChem (2021), 8(9), 1571-1573, database is CAplus.

An electrophotocatalytic method was developed for the dehydrogenative cross coupling of arenes with azoles employing a bicatalytic system consisting of acridinium dye and (2,2,6,6-tetramethylpiperidin-1-yl)oxyl (TEMPO). The reactions were conducted in a simple undivided cell with visible-light irradiation and requires no external chem. oxidant.

ChemElectroChem published new progress about 930-36-9. 930-36-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole, name is 1-Methylpyrazole, and the molecular formula is C4H6N2, HPLC of Formula: 930-36-9.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Li, He published the artcileStructural diversity and properties of four complexes with 4-acyl pyrazolone derivative, Recommanded Product: 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, the publication is Polyhedron (2013), 209-215, database is CAplus.

Four {[Zn(HL)(H₂O)(DMF)](NO₃)}_n (1), [Cd(HL)₂]_n (2), {[Mn(HL)₂]·MeCN·2H₂O} (3) and {[Mn(L)(μ₂-EtOH)]}_n (4) (H₂L = N-(1-phenyl-3-methyl-4-benzal-pyrazolone-5)-nicotinic hydrazide) were synthesized and characterized by elemental analyses, IR spectra, thermal analyses and single crystal x-ray diffraction. The structural analyses reveal that complexes 1, 2 and 3, formed by H₂L with metal nitrate, have Zigzag chain, double-stranded chain and mononuclear structures, resp., and the ligands adopt three different coordination modes in these complexes. While, complex 4, formed by H₂L with Mn acetate, represents a 2-dimensional network structure with dinuclear units bridged by EtOH mols. The metal atom and counteranion have certain influences on the structures of resulting complexes. The fluorescent properties of 1 and 2 and the magnetism of 4 were studied.

Polyhedron published new progress about 4551-69-3. 4551-69-3 belongs to pyrazoles-derivatives, auxiliary class Benzenes, name is 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, and the molecular formula is C17H14N2O2, Recommanded Product: 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Liu, Mei published the artcileSynthesis and SAR of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones as novel, selective c-Jun N-terminal kinase inhibitors, Safety of (1H-Pyrazol-5-yl)boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2006), 16(10), 2590-2594, database is CAplus and MEDLINE.

A novel class of 1,9-dihydro-9-hydroxypyrazolo[3,4-b]quinolin-4-ones I [R¹ = Me, Me₂CH, MeOCH₂CH₂, HO₂C(CH₂)₃, MeCONHCH₂CH₂, etc.; R² = Me, Et, Ph, HO₂CCH₂, HOCH₂CH₂, etc.; R³ = H, Cl, Ph, 3-pyrazolyl] as c-Jun-N-terminal kinase (JNK) inhibitors is described. These compounds were synthesized via the condensation of 2-nitrobenzaldehydes and hydroxypyrazoles. The structure-activity relationships (SAR) and kinase selectivity profile of the inhibitors are also discussed. Compound II was identified as a potent JNK inhibitor with good cellular potency.

Bioorganic & Medicinal Chemistry Letters published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Safety of (1H-Pyrazol-5-yl)boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Cai, Dongren published the artcileDesign and synthesis of novel Bronsted-Lewis acidic ionic liquid and its application in biodiesel production from soapberry oil, Related Products of pyrazoles-derivatives, the publication is Energy Conversion and Management (2018), 318-327, database is CAplus.

With the combination of mol. simulation and relevant experiments, the efficient Bronsted-Lewis acidic ionic liquid (IL) was designed and synthesized for biodiesel production from soapberry oil. In mol. simulation, 4-methylthiazole (MT) is proved to be the best matrix for IL preparation via electrostatic potential anal. and proton affinity anal., and it also is verified by experiments In orthogonal experiment, the relationship in catalytic activity between Bronsted-Lewis acidic IL and corresponding materials (Bronsted acidic IL and metal chloride) was revealed. Meanwhile, [Ps-MTH][CF₃SO₃] and FeCl₃ are verified as the best materials for preparation of Bronsted-Lewis acidic IL, and [Ps-MTH][CF₃SO₃]-FeCl₃(x = 0.65) is determined as the most efficient catalyst in the end. The Lewis acidity, Bronsted acidity and interaction of [Ps-MTH][CF₃SO₃] and FeCl₃ in [Ps-MTH][CF₃SO₃]-FeCl₃(x = 0.65) were characterized by FT-IR. And the catalytic mechanism of transesterification catalyzed by prepared IL was clarified. In order to maximize the biodiesel yield, optimization of process variables was conducted using Box-Behnken response surface methodol. The 97.04% of high biodiesel yield is obtained under the optimum conditions: reaction temperature was 127 °C, molar ratio (methanol to soapberry oil) was 27.96:1, catalyst amount was 3.06 mmol and reaction time was 8 h. Furthermore, [Ps-MTH][CF₃SO₃]-FeCl₃(x = 0.65) presents good catalytic activity in different transesterification for biodiesel production And its catalytic activity decreases from 97.04% to 93.59% after being used for 5 times, which reflects good reusability. The main properties of soapberry biodiesel were also measured and compared to the ASTM D6751 standard

Energy Conversion and Management published new progress about 930-36-9. 930-36-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole, name is 1-Methylpyrazole, and the molecular formula is C4H6N2, Related Products of pyrazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Dong, Dawei published the artcileCrosslinked anion exchange membranes with regional intensive ion clusters prepared from quaternized branched polyethyleneimine/quaternized polysulfone, Product Details of C4H6N2, the publication is International Journal of Hydrogen Energy (2022), 47(59), 24991-25006, database is CAplus.

A series of anion exchange membranes (AEMs) with regionally dense ion clusters are prepared by crosslinking quaternized polysulfone (QPSU) with quaternized branched polyethyleneimine (QBPEI). For the as-prepared QPSU/QBPEI AEMs, the hydrophilic QBPEI forms locally aggregated ion clusters in the QPSU matrix, which can promote the formation of an obvious microphase separation structure in the membrane. The QPSU/QBPEI-3 AEM with an ion exchange capacity of 1.88 meq/g exhibits the best performance, achieving a reasonably high ionic conductivity of 66.14 mS/cm at 80°C and showing good oxidation stability and alkali resistance. Finally, the maximum power d. of a single H₂/O₂ fuel cell with QPSU/QBPEI-3 AEM reaches 75.34 mW/cm² at 80°C. The above results indicate that QBPEI with a dendritic structure and abundant anionic conductive groups has a good application prospect in the preparation of AEMs with locally aggregated ion clusters and microphase separation structures.

International Journal of Hydrogen Energy published new progress about 930-36-9. 930-36-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole, name is 1-Methylpyrazole, and the molecular formula is C4H6N2, Product Details of C4H6N2.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Zhang, Qingwei published the artcileHit to Lead optimization of a novel class of squarate-containing polo-like kinase inhibitors, COA of Formula: C3H5BN2O2, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(24), 7615-7622, database is CAplus and MEDLINE.

Aminodioxocyclobutenylamino pyrimidineamines (aminopyrimidine squaramides) such as I, derived from a squaramide identified through high-throughput screening, were prepared as selective Polo-like kinase 1 (Plk1) inhibitors for potential use as antitumor agents. Using mol. modeling and extensive structure-activity studies, I (Plk1 K_i = 5 nM; EC₅₀ = 1.05 μM) was identified; its inhibition of Plk1 and of a panel of kinases, its lipophilicity, and its pharmacokinetics were determined I demonstrated moderate efficacy at dosages of 100 mg/kg in a murine pancreatic cancer xenograft tumor model and no overt toxicity.

Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C9H17NO, COA of Formula: C3H5BN2O2.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics