Category: 2051-95-8

Hua, Yun-Yu published the artcileIridium-Catalyzed Asymmetric Hydrogenation of γ- and δ-Ketoacids for Enantioselective Synthesis of γ- and δ-Lactones, Related Products of catalysis-chemistry, the publication is Organic Letters (2020), 22(3), 818-822, database is CAplus and MEDLINE.

A highly efficient asym. hydrogenation of γ- and δ-ketoacids was developed by using a chiral spiro iridium catalyst, affording the optically active γ- and δ-hydroxy acids/lactones in high yields with excellent enantioselectivities (up to >99% ee) and turnover numbers (TON up to 100000). This protocol provides an efficient and practical method for enantioselective synthesis of Ezetimibe.

Organic Letters published new progress about 2051-95-8. 2051-95-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ketone, name is 3-Benzoylpropionicacid, and the molecular formula is C10H10O3, Related Products of catalysis-chemistry.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Thomas, Nicholas C. published the artcilePreparation and Structures of Rare Earth 3-Benzoylpropanoates and 3-Phenylpropanoates, Application of 3-Benzoylpropionicacid, the publication is Australian Journal of Chemistry (2020), 73(12), 1250-1259, database is CAplus.

Rare earth (RE) complexes of 3-benzoylpropanoate (bp), [RE(bp)₃(H₂O)_n] (RE = La, n = 2; RE = Y, Ce, Pr, Nd, Yb, n = 1) and 3-phenylpropanoate (pp), [RE(pp)₃] (RE = Y, La, Ce, Nd, Yb), have been prepared by metathesis reactions between the corresponding rare earth chloride and the appropriate sodium carboxylate. Anal. by single-crystal x-ray diffraction finds that both RE bp and pp complexes favor formation of carboxylate-bridged 1-D coordination polymers in the solid state. Here, the former favors heteroleptic 9 or 10-coordinate complexes (splitting between Ce and La) with the carbonyl remaining uncoordinated but participating as a hydrogen bond acceptor with water in the coordination sphere. Lack of bp carbonyl coordination leaves this group available for surface interactions during corrosion inhibition and complex solubilization. The latter pp derivatives form eight-coordinate complexes for Y and Yb and are the first examples of homoleptic RE pp complexes to be reported.

Australian Journal of Chemistry published new progress about 2051-95-8. 2051-95-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ketone, name is 3-Benzoylpropionicacid, and the molecular formula is C18H20N2O12, Application of 3-Benzoylpropionicacid.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Espadinha, Margarida published the artcileTryptophanol-derived oxazolopyrrolidone lactams as potential anticancer agents against gastric adenocarcinoma, COA of Formula: C10H10O3, the publication is Pharmaceuticals (2021), 14(3), 208, database is CAplus and MEDLINE.

Gastric cancer is one of the deadliest cancers in modern societies, so there is a high level of interest in discovering new drugs for this malignancy. Previously, we demonstrated the ability of tryptophanol-derived polycyclic compounds to activate the tumor suppressor protein p53, a relevant therapeutic target in cancer. In this work, we developed a novel series of enantiomerically pure tryptophanol-derived small mols. to target human gastric adenocarcinoma (AGS) cells. From an initial screening of fourteen compounds in AGS cell line, a hit compound was selected for optimization, leading to two derivatives selective for AGS gastric cells over other types of cancer cells (MDA-MB-231, A-549, DU-145, and MG-63). More importantly, the compounds were non-toxic in normal cells (HEK 293T). Addnl., we show that the growth inhibition of AGS cells induced by these compounds is mediated by apoptosis. Stability studies in human plasma and human liver microsomes indicate that the compounds are stable, and that the major metabolic transformations of these mols. are mono- and di-hydroxylation of the indole ring.

Pharmaceuticals published new progress about 2051-95-8. 2051-95-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ketone, name is 3-Benzoylpropionicacid, and the molecular formula is C10H10O3, COA of Formula: C10H10O3.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Ates, Havva published the artcileAdvanced oxidation of landfill leachate: Removal of micropollutants and identification of by-products, Application In Synthesis of 2051-95-8, the publication is Journal of Hazardous Materials (2021), 125326, database is CAplus and MEDLINE.

Landfill leachate contains several macropollutants and micropollutants that cannot be removed efficiently by conventional treatment processes. Therefore, an advanced oxidation process is a promising step in post or pre-treatment of leachate. In this study, the effects of Fenton and ozone oxidation on the removal of 16 emerging micropollutants including polycyclic aromatic hydrocarbons (PAHs), phthalates, alkylphenols and pesticides were investigated. The Fenton and ozone oxidation of the leachate were performed with four (reaction time: 20-90 min, Fe(II) dose: 0.51-2.55 g/L, H₂O₂ dose: 5.1-25.5 g/L and pH: 3-5) and two (ozonation time: 10-130 min and pH: 4-10) independent variables, resp. Among these operating conditions, reaction time played more significant role (p-value < 0.05) in eliminating di-(2-Ethylhexyl) phthalate, 4-nonylphenol and 4-tert-octylphenol for both processes. The results showed that Fenton and ozone oxidation processes had a high degradation potential for micropollutants except for the PAHs including four and more rings. Removal efficiencies of micropollutants by ozone and Fenton oxidation were determined in the range of 5-100%. Although the removal efficiencies of COD (COD) and some micropollutants such as phthalates were found much higher in the Fenton process than ozonation, the degradation products occurred during the Fenton oxidation were a higher mol. weight Moreover, the oxidation intermediates for the both processes were found as mainly benzaldehyde, pentanoic acid and hydro cinnamic acid as well as derivatives of naphthalenone and naphthalenediol. Also, acid ester with higher mol. weight, naphthalene-based and phenolic compounds were detected in the Fenton oxidation

Journal of Hazardous Materials published new progress about 2051-95-8. 2051-95-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ketone, name is 3-Benzoylpropionicacid, and the molecular formula is C10H10O3, Application In Synthesis of 2051-95-8.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Lindstedt, Philip R. published the artcileEnhancement of the anti-aggregation activity of a molecular chaperone using a rationally designed post-translational modification, Related Products of catalysis-chemistry, the publication is ACS Central Science (2019), 5(8), 1417-1424, database is CAplus and MEDLINE.

Protein behavior is closely regulated by a plethora of post-translational modifications (PTMs). It is therefore desirable to develop approaches to design rational PTMs to modulate specific protein functions. Here, we report one such method, and we illustrate its successful implementation by potentiating the anti-aggregation activity of a mol. chaperone. Mol. chaperones are a multifaceted class of proteins essential to protein homeostasis, and one of their major functions is to combat protein misfolding and aggregation, a phenomenon linked to a number of human disorders. In this work, we conjugated a small-mol. inhibitor of the aggregation of α-synuclein, a process associated with Parkinson’s disease (PD), to a specific cysteine residue on human Hsp70, a mol. chaperone with five free cysteines. We show that this regioselective conjugation augments in vitro the anti-aggregation activity of Hsp70 in a synergistic manner. This Hsp70 variant also displays in vivo an enhanced suppression of α-synuclein aggregation and its associated toxicity in a Caenorhabditis elegans model of PD.

ACS Central Science published new progress about 2051-95-8. 2051-95-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ketone, name is 3-Benzoylpropionicacid, and the molecular formula is C10H10O3, Related Products of catalysis-chemistry.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Asif, Mohammad published the artcileIn silico activities, toxicity profiles and dug-like properties of some pyridazinyl benzenesulfonamides as a COX-inhibitor and antineoplastic agent, SDS of cas: 2051-95-8, the publication is Latin American Journal of Pharmacy (2021), 40(8), 1762-1769, database is CAplus.

This study was designed to predict in silico cyclooxygenase-2 (COX-2) inhibitory, antineoplastic activities, and toxicity profile of some benzenesulfonamide-pyridazinone derivatives, I [R = C₆H₅, 4-Me-C₆H₄, 4-Et-C₆H₄, etc] since COX-2 inhibitors have significant antineoplastic activity and cardiotoxicity. The result suggested that the biol. activity score has revealed that compounds I [R = 4-CO₂H-C₆H₄, 4-CHO-C₆H₄, 2-anthryl] have the highest protease enzyme inhibitory activity compare to standard drug celecoxib. All the compounds follow Lipinski’s rule of 5 except celecoxib and compound I [R = 2-anthryl]. Predicted ligand-target interaction has showed that celecoxib and compound I [R = 4-Br-C₆H₄] have COX-2 inhibitory activity. Compounds I [R = 4-Me-C₆H₄, 4-Et-C₆H₄,4-F-C₆H₄,4-Cl-C₆H₄, 4-Br-C₆H₄,4-I-C₆H₄, 4-EtO-C₆H₄, 2-naphthyl] targets the cell division control protein homologies with their specific E values. The remaining compounds were carbonic anhydrase inhibitors. Compound I [R = (4-phenylphenyl)] did not show any specific targets. Celecoxib, compound I [R = 4-I-C₆H₄, (4-acetylphenyl)] can act on breast ductal cell carcinoma with probability value (Pa) values0.640, 0.626, and 0.625, resp. Compound I [R = 4-methylbenzohydrazide] act on glioblastoma with Pa value of 0.667. The remaining compound act on non-small cell carcinoma with compound I [R = 4-I-C₆H₄] has a high Pa value of 0.760. All the compounds have the probability of hERG blocking activity except compound <I [R = (4-phenylphenyl)] . Compounds I [R = C₆H₅, 2-naphthyl] and Celecoxib have the highest blocking probability. All the compounds are showing hepatotoxicity among them compounds I [R = 4-Et-C₆H₄, 4-F-C₆H₄, 4-MeO-C₆H₄, 4-EtO-C₆H₄, 4-NH₂-C₆H₄, 4-CHO-C₆H₄, (4-acetylphenyl), (4-acetoxyphenyl), (4-carbamoylphenyl)] have the highest toxicity probability. All the compounds are Ames neg. As carbonic anhydrase enzyme is now a promising therapeutic target for cancer, the present compounds understudy may show promising activity as a COX inhibitor as well as anticancer compounds “CLC pred” results also strengthening our prediction that maximum compounds are better acting on non-small cell lung carcinoma (NSCLC).

Latin American Journal of Pharmacy published new progress about 2051-95-8. 2051-95-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ketone, name is 3-Benzoylpropionicacid, and the molecular formula is C10H10O3, SDS of cas: 2051-95-8.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Richard-Bildstein, Sylvia published the artcileDiscovery of the Potent, Selective, Orally Available CXCR7 Antagonist ACT-1004-1239, Related Products of catalysis-chemistry, the publication is Journal of Medicinal Chemistry (2020), 63(24), 15864-15882, database is CAplus and MEDLINE.

The chemokine receptor CXCR7, also known as ACKR3, is a seven-transmembrane G-protein-coupled receptor (GPCR) involved in various pathologies such as neurol. diseases, autoimmune diseases, and cancers. By binding and scavenging the chemokines CXCL11 and CXCL12, CXCR7 regulates their extracellular levels. From an original high-throughput screening campaign emerged an arylketoamide hit among others. The hit-to-lead optimization led to the discovery of a novel chemotype series of acylaminopiperidinecarboxamides. This series provided CXCR7 antagonists that block CXCL11- and CXCL12-induced ss-arrestin recruitment. Further structural modifications on the acylaminopiperidinecarboxamide framework yielded compounds with high CXCR7 antagonistic activities and balanced ADMET properties. The effort described herein culminated in the discovery of ACT-1004-1239 I. Biol. characterization of I demonstrated that it is a potent, insurmountable antagonist. Oral administration of I in mice up to 100 mg/kg led to a dose-dependent increase of plasma CXCL12 concentration

Journal of Medicinal Chemistry published new progress about 2051-95-8. 2051-95-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ketone, name is 3-Benzoylpropionicacid, and the molecular formula is C10H10O3, Related Products of catalysis-chemistry.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Gad, Nourhan M. published the artcileReactivity of 5-phenyl-3-[(2-chloroquinolin-3-yl)methylene]furan-2(3H)-one towards hydrazine and benzylamine: A comparative study, Application In Synthesis of 2051-95-8, the publication is Synthetic Communications (2021), 51(9), 1384-1397, database is CAplus.

The reactivity of a 2-chloroquinolinylfuranone derivative was investigated against two nitrogen nucleophilic reagents namely, hydrazine and benzylamine. It was found that the regioselectivity of the reaction products was mainly dependent on the nature of nucleophiles, reaction conditions and solvent used. Therefore, hydrazinolysis of afforded the corresponding acid hydrazide and pyridazinone derivatives depending on the reaction conditions. Otherwise, benzylamine reacted with at different reaction aspects to provide N-benzylamide, N-benzylpyrrolone, and 2-benzylaminoquinolinyl-N-benzylpyrrolone derivatives The chem. structures of all synthesized compounds were substantiated from their anal. as well as spectroscopic data. Based on the charge d. calculations and computational chem. study which excluded the aza-Michael addition reaction and confirm the higher electron-deficiency of lactone carbonyl group than C2-quinoline position, it could be concluded that the C2-furanone becomes more susceptible to attack by the nucleophilic reagent, hydrazine and benzylamine.

Synthetic Communications published new progress about 2051-95-8. 2051-95-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ketone, name is 3-Benzoylpropionicacid, and the molecular formula is C10H10O3, Application In Synthesis of 2051-95-8.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Abdelbaset, Mahmoud S. published the artcileDesign, synthesis, and biological evaluation of new series of pyrrol-2(3H)-one and pyridazin-3(2H)-one derivatives as tubulin polymerization inhibitors, Related Products of catalysis-chemistry, the publication is Bioorganic Chemistry (2021), 104522, database is CAplus and MEDLINE.

A potential microtubule destabilizing series of new thirty-five Pyrrol-2-one, Pyridazin-3(2H)-one and Pyridazin-3(2H)-one/oxime derivatives has been synthesized and tested for their antiproliferative activity against a panel of 60 human cancer cell lines. Compounds IVc, IVg and IVf showed a broad spectrum of growth inhibitory activity against cancer cell lines representing renal, cancer of lung, colon, central nervous system, ovary, and kidney. Among them, compound IVg was found to have broad spectrum anti-tumor activity against the tested nine tumor subpanels with selectivity ratios ranging between 0.21 and 3.77 at the GI50 level. In vitro assaying revealed tubulin polymerization inhibition by all active compounds IVc, IVg and IVf. The results of the docking study revealed nice fitting of compounds IVc, IVf, and IVg into CA-4 binding site in tubulin. The three compounds exhibited high binding affinities (ΔGb = -12.49 to -12.99 kcal/mol) toward tubulin compared to CA-4 (-8.87 kcal/mol). Investigation of the binding modes of the three compounds IVc, IVf, and IVg revealed that they interacted mainly hydrophobically with tubulin and similar binding orientations to that of CA-4. These observations suggest that tubulin is a possible target for these compounds

Bioorganic Chemistry published new progress about 2051-95-8. 2051-95-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ketone, name is 3-Benzoylpropionicacid, and the molecular formula is C10H10O3, Related Products of catalysis-chemistry.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia