Day: September 16, 2022

Giereth, Robin;Mengele, Alexander K.;Frey, Wolfgang;Kloss, Marvin;Steffen, Andreas;Karnahl, Michael;Tschierlei, Stefanie published 《Copper(I) Phosphinooxazoline Complexes: Impact of the Ligand Substitution and Steric Demand on the Electrochemical and Photophysical Properties》 in 2020. The article was appeared in 《Chemistry – A European Journal》. They have made some progress in their research.Recommanded Product: (S)-2-(2-(Diphenylphosphanyl)phenyl)-4-isobutyl-4,5-dihydrooxazole The article mentions the following:

Seven homoleptic Cu^I complexes based on hetero-bidentate PN̂ ligands were synthesized and comprehensively characterized. To study structure-property relations, the type, size, number and configuration of substituents at the phosphinooxazoline (phox) ligands were systematically varied. To this end, a combination of x-ray diffraction, NMR spectroscopy, steady-state absorption and emission spectroscopy, time-resolved emission spectroscopy, quenching experiments and cyclic voltammetry was used to assess the photophys. and electrochem. properties. Also, time-dependent d. functional theory calculations were applied to also analyze the excited state structures and characteristics. Surprisingly, a strong dependency on the chirality of the resp. PN̂ ligand was found, whereas the specific kind and size of the different substituents has only a minor impact on the properties in solution Most importantly, all complexes except C3 are photostable in solution and show fully reversible redox processes. Sacrificial reductants were applied to demonstrate a successful electron transfer upon light irradiation These properties render this class of photosensitizers as potential candidates for solar energy conversion issues. And (S)-2-(2-(Diphenylphosphanyl)phenyl)-4-isobutyl-4,5-dihydrooxazole (cas: 167693-62-1) was used in the research process.

(S)-2-(2-(Diphenylphosphanyl)phenyl)-4-isobutyl-4,5-dihydrooxazole(cas: 167693-62-1) is a compound of chiral-phosphine-ligands. At present, the synthesis of new chiral phosphines designed specifically for nucleophilic organocatalysis remains a significant challenge.Recommanded Product: (S)-2-(2-(Diphenylphosphanyl)phenyl)-4-isobutyl-4,5-dihydrooxazole

Reference:
Phosphine ligand,
Chiral phosphines in nucleophilic organocatalysis

Recommanded Product: 34031-32-8《The thioredoxin reductase inhibitor auranofin suppresses pulmonary metastasis of osteosarcoma, but not local progression》 was published in 2021. The authors were Kinoshita, Hideyuki;Shimozato, Osamu;Ishii, Takeshi;Kamoda, Hiroto;Hagiwara, Yoko;Tsukanishi, Toshinori;Ohtori, Seiji;Yonemoto, Tsukasa, and the article was included in《Anticancer Research》. The author mentioned the following in the article:

Auranofin (AUR), a thioredoxin reductase (TXNRD) inhibitor, shows anticancer activity against several cancers. This study investigated the effects of AUR on the local progression and pulmonary metastasis of osteosarcoma (OS). Publicly available expression cohorts were analyzed to study the relationship between TXNRD-2 expression and the survival of patients with OS. The murine OS cell line LM8 was stimulated with AUR. Cell viability, apoptosis-related protein levels, caspase activity, and wound healing were analyzed. Tumor progression and pulmonary metastasis were investigated in C3H mice implanted with LM8 cells. High-level expression of TXNRD-2 represented a neg. prognostic factor for metastasis and overall survival in patients with OS. AUR induced apoptosis of OS cells via the oxidative stress-MAPK-Caspase 3 pathway, and suppressed the migration of OS cells. AUR inhibited the pulmonary metastasis of OS, but not local progression. AUR represents a potential therapeutic drug for suppressing pulmonary metastasis of OS. The experimental procedure involved many compounds, such as ((2S,3R,4S,5R,6R)-3,4,5-Triacetoxy-6-(acetoxymethyl)tetrahydro-2H-pyran-2-thio)(triethylphosphine)gold (cas: 34031-32-8) .

((2S,3R,4S,5R,6R)-3,4,5-Triacetoxy-6-(acetoxymethyl)tetrahydro-2H-pyran-2-thio)(triethylphosphine)gold(cas: 34031-32-8) is an efficient inducer of mitochondrial membrane permeability transition pore in the presence of calcium ions related to its inhibition of mitochondrial thioredoxin reductase.Recommanded Product: 34031-32-8

Reference:
Phosphine ligand,
Chiral phosphines in nucleophilic organocatalysis

Enriquez-Flores, Sergio;Flores-Lopez, Luis A.;De la Mora-De la Mora, Ignacio;Garcia-Torres, Itzhel;Gracia-Mora, Isabel;Gutierrez-Castrellon, Pedro;Fernandez-Lainez, Cynthia;Martinez-Perez, Yoalli;Olaya-Vargas, Alberto;de Vos, Paul;Lopez-Velazquez, Gabriel published 《Naturally occurring deamidated triosephosphate isomerase is a promising target for cell-selective therapy in cancer》. The research results were published in《Scientific Reports》 in 2022.COA of Formula: C20H36AuO9PS The article conveys some information:

Human triosephosphate isomerase (HsTIM) is a central glycolytic enzyme and is overexpressed in cancer cells with accelerated glycolysis. Triple-neg. breast cancer is highly dependent on glycolysis and is typically treated with a combination of surgery, radiation therapy, and chemotherapy. Deamidated HsTIM was recently proposed as a druggable target. Although thiol-reactive drugs affect cell growth in deamidated HsTIM-complemented cells, the role of this protein as a selective target has not been demonstrated. To delve into the usefulness of deamidated HsTIM as a selective target, we assessed its natural accumulation in breast cancer cells. We found that deamidated HsTIM accumulates in breast cancer cells but not in noncancerous cells. The cancer cells are selectively programmed to undergo cell death with thiol-reactive drugs that induced the production of methylglyoxal (MGO) and advanced glycation-end products (AGEs). In vivo, a thiol-reactive drug effectively inhibits the growth of xenograft tumors with an underlying mechanism involving deamidated HsTIM. Our findings demonstrate the usefulness of deamidated HsTIM as target to develop new therapeutic strategies for the treatment of cancers and other pathologies in which this post translationally modified protein accumulates.((2S,3R,4S,5R,6R)-3,4,5-Triacetoxy-6-(acetoxymethyl)tetrahydro-2H-pyran-2-thio)(triethylphosphine)gold (cas: 34031-32-8) were involved in the experimental procedure.

((2S,3R,4S,5R,6R)-3,4,5-Triacetoxy-6-(acetoxymethyl)tetrahydro-2H-pyran-2-thio)(triethylphosphine)gold(cas: 34031-32-8) is a potent inhibitor of selenoenzyme thioredoxin reductase (TrxR), which is involved in defense against oxidative stress.COA of Formula: C20H36AuO9PS

Reference:
Phosphine ligand,
Chiral phosphines in nucleophilic organocatalysis

Koch, Guido;Lloyd-Jones, Guy C.;Loiseleur, Olivier;Pfaltz, Andreas;Pretot, Roger;Schaffner, Siliva;Schnider, Patrick;von Matt, Peter published 《Synthesis of chiral (phosphinoaryl)oxazolines, a versatile class of ligands for asymmetric catalysis》. The research results were published in《Recueil des Travaux Chimiques des Pays-Bas》 in 1995.Recommanded Product: 167693-62-1 The article conveys some information:

Enantiomerically pure 2-[2-(diphenylphosphino)aryl]oxazolines I (R = Ph, CHMe₂, CMe₃, CH₂Ph, isobutyl) are readily prepared from 2-bromobenzonitrile by transmetalation with BuLi, subsequent reaction with chlorodiphenylphosphine and conversion of the resulting phosphinoaryl nitrile to the oxazoline by treatment with a chiral amino alc. in the presence of ZnCl₂. An alternative synthesis is based on the ortho-metalation of 2-aryloxazolines followed by reaction with chlorodiphenylphosphine.(S)-2-(2-(Diphenylphosphanyl)phenyl)-4-isobutyl-4,5-dihydrooxazole (cas: 167693-62-1) were involved in the experimental procedure.

(S)-2-(2-(Diphenylphosphanyl)phenyl)-4-isobutyl-4,5-dihydrooxazole(cas: 167693-62-1) is a compound of chiral-phosphine-ligands. At present, the synthesis of new chiral phosphines designed specifically for nucleophilic organocatalysis remains a significant challenge.Recommanded Product: 167693-62-1

Reference:
Phosphine ligand,
Chiral phosphines in nucleophilic organocatalysis

Recommanded Product: 34031-32-8In 2021, Isei, Michael O.;Stevens, Don;Kamunde, Collins published 《Temperature rise and copper exposure reduce heart mitochondrial reactive oxygen species scavenging capacity》. 《Comparative Biochemistry and Physiology, Part C: Toxicology & Pharmacology》published the findings. The article contains the following contents:

Mitochondria produce and scavenge reactive oxygen species (ROS); however, whether oxidative distress due to exogenous stress arises from excessive production or impaired scavenging remains unclear. We assessed the effect of copper (Cu) and thermal stress on kinetics of ROS (H2O2) consumption in mitochondria isolated from fish heart. Mitochondria were energized with succinate, glutamate-malate or palmitoylcarnitine (PC) and incubated with 1-25μM Cu at 11 (control) and 23°C. We found that H2O2 consumption capacity of heart mitochondria varies with substrate and is additively reduced by temperature rise and Cu. While Cu is a potent inhibitor of H2O2 consumption in mitochondria oxidizing glutamate-malate and succinate, mitochondria oxidizing PC are resistant to the inhibitory effect of the metal. Moreover, the sensitivity of H2O2 consumption pathways to Cu depend on the substrate and are greatly impaired during oxidation of glutamate-malate. Pharmacol. manipulation of mitochondrial antioxidant systems revealed that NADPH-dependent peroxidase systems are the centerpieces of ROS scavenging in heart mitochondria, with the glutathione-dependent pathway being the most prominent while catalase played a minimal role. Surprisingly, Cu is as efficacious in inhibiting thioredoxin-dependent peroxidase pathway as auranofin, a selective inhibitor of thioredoxin reductase. Taken together, our study uncovered unique mechanisms by which Cu alters mitochondrial H2O2 homeostasis including its ability to inhibit specific mitochondrial ROS scavenging pathways on a par with conventional inhibitors. Importantly, because of additive inhibitory effect on mitochondrial ROS removal mechanisms, hearts of organisms jointly exposed to Cu and thermal stress are likely at increased risk of oxidative distress. The experimental procedure involved many compounds, such as ((2S,3R,4S,5R,6R)-3,4,5-Triacetoxy-6-(acetoxymethyl)tetrahydro-2H-pyran-2-thio)(triethylphosphine)gold (cas: 34031-32-8) .

((2S,3R,4S,5R,6R)-3,4,5-Triacetoxy-6-(acetoxymethyl)tetrahydro-2H-pyran-2-thio)(triethylphosphine)gold(cas: 34031-32-8) is a gold(I)-phosphine thiolate small molecule described to produce antiinflammatory and antiarthritic effects.Recommanded Product: 34031-32-8

Reference:
Phosphine ligand,
Chiral phosphines in nucleophilic organocatalysis

Ito, Kan;Nishida, Yoshihiro;Hamada, Shunsuke;Shimizu, Koki;Sakai, Tomohisa;Ohkawara, Bisei;Alman, Benjamin A.;Enomoto, Atsushi;Ikuta, Kunihiro;Koike, Hiroshi;Zhang, Jiarui;Ohno, Kinji;Imagama, Shiro published 《Efficacy of auranofin as an inhibitor of desmoid progression》. The research results were published in《Scientific Reports》 in 2022.Formula: C20H36AuO9PS The article conveys some information:

Abstract: Anticancer drugs and mol. targeted therapies are used for refractory desmoid-type fibromatosis (DF), but occasionally cause severe side effects. The purpose of this study was to identify an effective drug with fewer side effects against DF by drug repositioning, and evaluate its efficacy. FDA-approved drugs that inhibit the proliferation of DF cells harboring S45F mutations of CTNNB1 were screened. An identified drug was subjected to the investigation of apoptotic effects on DF cells with anal. of Caspase 3/7 activity. Expression of β-catenin was evaluated with western blot anal., and immunofluorescence staining. Effects of the identified drug on in vivo DF were analyzed using Apc1638N mice. Auranofin was identified as a drug that effectively inhibits the proliferation of DF cells. Auranofin did not affect Caspase 3/7 activity compared to control. The expression level of β-catenin protein was not changed regardless of auranofin concentration Auranofin effectively inhibited the development of tumorous tissues by both oral and i.p. administration, particularly in male mice. Auranofin, an anti-rheumatic drug, was identified to have repositioning effects on DF. Since auranofin has been used for many years as an FDA-approved drug, it could be a promising drug with fewer side effects for DF. To complete the study, the researchers used ((2S,3R,4S,5R,6R)-3,4,5-Triacetoxy-6-(acetoxymethyl)tetrahydro-2H-pyran-2-thio)(triethylphosphine)gold (cas: 34031-32-8) .

((2S,3R,4S,5R,6R)-3,4,5-Triacetoxy-6-(acetoxymethyl)tetrahydro-2H-pyran-2-thio)(triethylphosphine)gold(cas: 34031-32-8) is a disease-modifying antirheumatic drug (DMARD) and has been used to study the anti-proliferative effects against OVCAR-3 human ovarian carcinoma cells.Formula: C20H36AuO9PS

Reference:
Phosphine ligand,
Chiral phosphines in nucleophilic organocatalysis

Versleijen, Jos P. G.;Van Leusen, Albert M.;Feringa, Ben L. published 《Copper(I) phosphoramidite catalyzed asymmetric conjugate addition of dialkylzinc reagents to α,β-unsaturated nitroacetates; an enantioselective route to β-aryl-nitroalkanes》. The research results were published in《Tetrahedron Letters》 in 1999.Computed Properties of C38H34NO2P The article conveys some information:

The asym. copper(I) phosphoramidite catalyzed conjugate addition of dialkylzinc reagents to E,Z-mixtures of α,β-unsaturated nitroacetates provided the 1,4-adducts in excellent yields but with low e.e.’s. High enantioselectivities (e.e.’s up to 92%) were obtained with structurally rigid 3-nitrocoumarins, leading to a new route to optically active β-aryl-nitroalkanes. And (11bS)-2,6-Dimethyl-N,N-bis(1-phenylethyl)dinaphtho[2,1-d:1′,2′-f][1,3,2]dioxaphosphepin-4-amine (cas: 201732-49-2) was used in the research process.

(11bS)-2,6-Dimethyl-N,N-bis(1-phenylethyl)dinaphtho[2,1-d:1′,2′-f][1,3,2]dioxaphosphepin-4-amine(cas: 201732-49-2) is a compound of chiral-phosphine-ligands. At present, the synthesis of new chiral phosphines designed specifically for nucleophilic organocatalysis remains a significant challenge.Computed Properties of C38H34NO2P

Reference:
Phosphine ligand,
Chiral phosphines in nucleophilic organocatalysis

Computed Properties of C20H36AuO9PS《Oxidative stress inducers potentiate 2,3,7,8-tetrachlorodibenzo-p-dioxin-mediated pre-cardiac edema in larval zebrafish》 was published in 2021. The authors were Tanaka, Katsuki;Adachi, Hikaru;Akasaka, Hironobu;Tamaoki, Junya;Fuse, Yuji;Kobayashi, Makoto;Kitazawa, Takio;Teraoka, Hiroki, and the article was included in《Journal of Veterinary Medical Science》. The author mentioned the following in the article:

We reported the involvement of oxidative stress and prostaglandins including thromboxane and prostacyclin in pre-cardiac edema (early edema) caused by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD). While the involvement of oxidative stress in TCDDinduced toxicity has been frequently reported, the mechanism of its action is still unclear. In the present study, oxidative stress inducers including paraquat, hydrogen peroxide (H₂O₂) and rotenone augmented early edema (edema) induced by a low concentration of TCDD (0.1 ppb) at 55 h post fertilization (hpf), while each of them alone did not cause edema. Edema caused by TCDD plus oxidative stress inducers was almost abolished by antioxidants, an antagonist for thromboxane receptor (ICI-192,605) and an agonist for prostacyclin receptor (beraprost), suggesting that the site of action of these inducers was in the regular signaling pathway after activation of aryl hydrocarbon receptor type 2 (AHR2) by TCDD. Oxidative stress inducers also enhanced edema caused by an agonist for the thromboxane receptor (U46619), and the enhancement was also inhibited by antioxidants. Sulforaphane and auranofin, activators of Nrf2 that is a master regulator of anti-oxidative response, did not affect U46619-evoked edema but almost abolished TCDD-induced edema and potentiation by paraquat in both TCDD- and U46619- induced edema. Taken together, the results suggest that oxidative stress augments pre-cardiac edema caused by TCDD via activation of thromboxane receptor-mediated signaling in developing zebrafish. As paraquat and other oxidative stress inducers used also are environmental pollutants, interaction between dioxin-like compounds and exogenous source of oxidative stress should also be considered. The experimental procedure involved many compounds, such as ((2S,3R,4S,5R,6R)-3,4,5-Triacetoxy-6-(acetoxymethyl)tetrahydro-2H-pyran-2-thio)(triethylphosphine)gold (cas: 34031-32-8) .

((2S,3R,4S,5R,6R)-3,4,5-Triacetoxy-6-(acetoxymethyl)tetrahydro-2H-pyran-2-thio)(triethylphosphine)gold(cas: 34031-32-8) is an efficient inducer of mitochondrial membrane permeability transition pore in the presence of calcium ions related to its inhibition of mitochondrial thioredoxin reductase.Computed Properties of C20H36AuO9PS

Reference:
Phosphine ligand,
Chiral phosphines in nucleophilic organocatalysis

Chakraborty, Parichita;Oosterhuis, Dorenda;Bonsignore, Riccardo;Casini, Angela;Olinga, Peter;Scheffers, Dirk-Jan published 《An Organogold Compound as Potential Antimicrobial Agent against Drug-Resistant Bacteria: Initial Mechanistic Insights》 in 2021. The article was appeared in 《ChemMedChem》. They have made some progress in their research.Product Details of 34031-32-8 The article mentions the following:

The rise of antimicrobial resistance has necessitated novel strategies to efficiently combat pathogenic bacteria. Metal-based compounds have been proven as a possible alternative to classical organic drugs. Here, we have assessed the antibacterial activity of seven gold complexes of different families. One compound, a cyclometalated Au(III) CN complex, showed activity against Gram-pos. bacteria, including multi-drug resistant clin. strains. The mechanism of action of this compound was studied in Bacillus subtilis. Overall, the studies point towards a complex mode of antibacterial action, which does not include induction of oxidative stress or cell membrane damage. A number of genes related to metal transport and homeostasis were upregulated upon short treatment of the cells with gold compound Toxicity tests conducted on precision-cut mouse tissue slices ex vivo revealed that the organogold compound is poorly toxic to mouse liver and kidney tissues, and may thus, be treated as an antibacterial drug candidate. The experimental procedure involved many compounds, such as ((2S,3R,4S,5R,6R)-3,4,5-Triacetoxy-6-(acetoxymethyl)tetrahydro-2H-pyran-2-thio)(triethylphosphine)gold (cas: 34031-32-8) .

((2S,3R,4S,5R,6R)-3,4,5-Triacetoxy-6-(acetoxymethyl)tetrahydro-2H-pyran-2-thio)(triethylphosphine)gold(cas: 34031-32-8) is an efficient inducer of mitochondrial membrane permeability transition pore in the presence of calcium ions related to its inhibition of mitochondrial thioredoxin reductase.Product Details of 34031-32-8

Reference:
Phosphine ligand,
Chiral phosphines in nucleophilic organocatalysis

Recommanded Product: 34031-32-8《Repurposing of Auranofin Against Bacterial Infections: An In silico and In vitro Study》 was published in 2021. The authors were Sharma, Nidhi;Singh, Arti;Sharma, Ruchika;Kumar, Anoop, and the article was included in《Current Computer-Aided Drug Design》. The author mentioned the following in the article:

The aim of the study was to find out the role of auranofin as a promising broadspectrum antibacterial agent. In vitro assays (Percentage growth retardation, Bacterial growth kinetics, Biofilm formation assay) and In silico study (Molegro virtual docker (MVD) version 6.0 and Mol. operating environment (MOE) version 2008.10 software). The in vitro assays have shown that auranofin has good antibacterial activity against Gram pos. and Gram neg. bacterial strains. Further, auranofin has shown synergistic activity in combination with ampicillin against S. aureus and B. subtilis whereas in combination with neomycin has just shown additive effect against E. coli, P. aeruginosa and B. pumilus. In vivo results have revealed that auranofin alone and in combination with standard drugs significantly decreased the bioburden in the zebrafish infection model as compared to control. The mol. docking study have shown good interaction of auranofin with penicillin-binding protein (2Y2M), topoisomerase (3TTZ), UDP-3-O-[3-hydroxymyristoyl] N-acetylglucosaminedeacetylase (3UHM), cell adhesion protein (4QRK), β-lactamase (5CTN) and arylsulphatase (1HDH) enzyme as that of reference ligand which indicate the multimodal mechanism of action of auranofin. Finally, MTT assay has shown the non-cytotoxic effect of auranofin. In conclusion, auranofin in combination with existing antibiotics, could be developed as a broad spectrum antibacterial agent; however, further studies are required to confirm its safety and efficacy. This study provides the possibility of the use of auranofin apart from its established therapeutic indication in combination with existing antibiotics to tackle the problem of resistance.((2S,3R,4S,5R,6R)-3,4,5-Triacetoxy-6-(acetoxymethyl)tetrahydro-2H-pyran-2-thio)(triethylphosphine)gold (cas: 34031-32-8) were involved in the experimental procedure.

((2S,3R,4S,5R,6R)-3,4,5-Triacetoxy-6-(acetoxymethyl)tetrahydro-2H-pyran-2-thio)(triethylphosphine)gold(cas: 34031-32-8) is a gold(I)-phosphine thiolate small molecule described to produce antiinflammatory and antiarthritic effects.Recommanded Product: 34031-32-8

Reference:
Phosphine ligand,
Chiral phosphines in nucleophilic organocatalysis