Category: 51656-68-9

Jiang, Wanlong published the artcileArylpropionylpiperazines as antagonists of the human melanocortin-4 receptor, Recommanded Product: 3-(2,6-Dichlorophenyl)propanoic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2006), 16(17), 4674-4678, database is CAplus and MEDLINE.

A series of 3-arylpropionylpiperazines were synthesized as antagonists of the melanocortin-4 receptor. Their potency was increased by replacing the α-Me substituent of the initial lead with a larger s-Bu or i-Bu group. Further potency enhancement was observed when a glycine or β-alanine was incorporated onto the benzylamine. Some compounds demonstrated good potency, moderate selectivity, and oral bioavailability.

Bioorganic & Medicinal Chemistry Letters published new progress about 51656-68-9. 51656-68-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene, name is 3-(2,6-Dichlorophenyl)propanoic acid, and the molecular formula is C9H8Cl2O2, Recommanded Product: 3-(2,6-Dichlorophenyl)propanoic acid.

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

Min, Kyung-Lyum published the artcileSynthesis and differential properties of creatine analogs as inhibitors for human creatine kinase isoenzymes, Related Products of chlorides-buliding-blocks, the publication is European Journal of Biochemistry (1996), 238(2), 446-452, database is CAplus and MEDLINE.

Fourteen new creatine analogs, all with a guanidine function and either a polar or an apolar group instead of the creatine carboxylic function, were tested as potential inhibitors for human creatine kinase by kinetic anal. of their effects on the reaction rate. Only compounds bearing an apolar aromatic moiety, which was spaced from the guanidine function by at least two bonds, proved to have a significant inhibitory activity and showed a mixed-type inhibition similar to that of creatine. Among these compounds, 2,6-dichlorobenzylguanidine (K_i = 5.6 mM and 39.8 mM for muscle-type and brain-type creatine kinases, resp.) and 3-(2,6-dichlorophenyl)propylguanidine (K_i = 15 mM and 4.5 mM) were the more potent inhibitors and showed a significant isoenzyme selectivity between muscle- and brain-type creatine kinases. Our results are in agreement with recent data that suggest the location of a hydrophobic pocket near the guanidine-binding domain of the enzyme. The observed selectivity in isoenzyme inhibition may be useful to study structural differences in catalytic centers.

European Journal of Biochemistry published new progress about 51656-68-9. 51656-68-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene, name is 3-(2,6-Dichlorophenyl)propanoic acid, and the molecular formula is C9H8Cl2O2, Related Products of chlorides-buliding-blocks.

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

Ramesh, Perla published the artcileRecyclable Aliphatic Nitrile-Template Enabled Remote meta-C-H Functionalization at Room Temperature, Synthetic Route of 51656-68-9, the publication is Journal of Organic Chemistry, database is CAplus and MEDLINE.

This article describes the development of a new aliphatic nitrile-template-directed remote meta-selective C-H olefin functionalization reaction of arenes. Remarkably, unlike the previous reports, this process was feasible at room temperature and enabled the formation of products with excellent regio-selectivity. The present protocol encompasses a broad spectrum of substituted dihydrocinnamic acids and olefins, producing meta-C-H olefinated products (up to 96% yield). In addition, the efficacy of the present method was showcased by the synthesis of various drug analogs (e.g., cholesterol, estrone, ibuprofen, and naproxen). Significantly, the robustness of meta-olefination was also demonstrated by gram-scale synthesis. The new nitrile-based meta-directing template, in particular, could be easily synthesized in two steps and recycled under mild conditions. A, B, and C represent the Intrinsic Reaction Curves (IRCs) for the meta-C-H activation, Alkene Insertion, and β-Hydride elimination, resp., along with the corresponding transition states. CYL view software was used for showing transition state structures.

Journal of Organic Chemistry published new progress about 51656-68-9. 51656-68-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene, name is 3-(2,6-Dichlorophenyl)propanoic acid, and the molecular formula is C9H8Cl2O2, Synthetic Route of 51656-68-9.

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

Chamberlain, K. published the artcileStudies on plant growth-regulating substances. LV. The plant growth-promoting properties of some β-aryl-propionic acids, SDS of cas: 51656-68-9, the publication is Annals of Applied Biology (1978), 90(1), 115-19, database is CAplus.

Of 17β-arylpropionic acids prepared and tested for their plant growth-regulating activity in wheat coleoptile, pea segment, and pea curvature tests, the following compounds were among the most active: β-(4-fluorophenyl) [459-31-4], β-(2,4-dichlorophenyl) [55144-92-8], and β-(2,6-dichlorophenyl)propionic acid [51656-68-9]. Of 4 other compounds of the general formula I (X = CH₂, O, NH, or S) which were also tested in this study, 2,4-D (I; X = O) [94-75-7] was generally the most active.

Annals of Applied Biology published new progress about 51656-68-9. 51656-68-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene, name is 3-(2,6-Dichlorophenyl)propanoic acid, and the molecular formula is C9H8Cl2O2, SDS of cas: 51656-68-9.

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

Chantler, Thomas published the artcileProximity effects in the electron impact mass spectra of 2-substituted benzazoles, SDS of cas: 51656-68-9, the publication is International Journal of Mass Spectrometry (2004), 236(1-3), 65-80, database is CAplus.

The 70 eV electron impact mass spectra of a wide range of 2-substituted benzazoles are reported and discussed. Particular attention is paid to the mechanistic significance and anal. utility of [M-H]⁺ and [M-X]⁺ signals in the spectra of benzazoles in which the 2-substituent contains a terminal aryl group with one or more substituents, X. Loss of H^• or X^• occurs preferentially from an ortho-position from ionized 2-benzylbenzimidazoles, 2-phenethylbenzimidazoles, 2-styrylbenzimidazoles, 2-styrylbenzoxazoles and 2-styrylbenzothiazoles. In the three styrylbenzazole series, the [M-H]⁺ and/or [M-X]⁺ signals dominate the spectra. This unusually facile loss of H^• or X^• may be attributed to a proximity effect, in which cyclization of the ionized mol. is followed by elimination of an ortho-substituent to give an exceptionally stable polycyclic ion. Formation of a new five- or six-membered ring by the proximity effect occurs rapidly; cyclization to a seven-membered ring takes place rather less readily; but formation of a ring with only four atoms or more than seven atoms is not observed to a significant extent. The proximity effect competes effectively with loss of a Me radical by simple cleavage of an Et, iso-Pr and even a t-Bu group in the pendant aromatic ring of ionized 2-(4-alkylstyryl)benzazoles.

International Journal of Mass Spectrometry published new progress about 51656-68-9. 51656-68-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene, name is 3-(2,6-Dichlorophenyl)propanoic acid, and the molecular formula is C9H8Cl2O2, SDS of cas: 51656-68-9.

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

Shultz, Michael D. published the artcileStructure-efficiency relationship of [1,2,4]triazol-3-ylamines as novel nicotinamide isosteres that inhibit tankyrases, Application of 3-(2,6-Dichlorophenyl)propanoic acid, the publication is Journal of Medicinal Chemistry (2013), 56(17), 7049-7059, database is CAplus and MEDLINE.

Tankyrases 1 and 2 are members of the poly(ADP-ribose) polymerase (PARP) family of enzymes that modulate Wnt pathway signaling. While amide- and lactam-based nicotinamide mimetics that inhibit tankyrase activity, such as XAV939, are well-known, the discovery and evaluation of a novel nicotinamide isostere that demonstrates selectivity over other PARP family members is reprted. The utilization of lipophilic efficiency-based structure-efficiency relationships (SER) to rapidly drive the evaluation of this series is demonstrated. These efforts led to a series of selective, cell-active compounds with solubility, physicochem., and in vitro properties suitable for further optimization.

Journal of Medicinal Chemistry published new progress about 51656-68-9. 51656-68-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene, name is 3-(2,6-Dichlorophenyl)propanoic acid, and the molecular formula is C15H19BO2, Application of 3-(2,6-Dichlorophenyl)propanoic acid.

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

Guo, Chuangxing published the artcileStructure-based design of novel human Pin1 inhibitors (III): Optimizing affinity beyond the phosphate recognition pocket, Application In Synthesis of 51656-68-9, the publication is Bioorganic & Medicinal Chemistry Letters (2014), 24(17), 4187-4191, database is CAplus and MEDLINE.

The design of potent Pin1 inhibitors has been challenging because its active site specifically recognizes a phospho-protein epitope. The de novo design of phosphate-based Pin1 inhibitors focusing on the phosphate recognition pocket and the successful replacement of the phosphate group with a carboxylate have been previously reported. The potency of the carboxylate series is now further improved through structure-based optimization of ligand-protein interactions in the proline binding site which exploits the H-bond interactions necessary for Pin1 catalytic function. Further optimization using a focused library approach led to the discovery of low nanomolar non-phosphate small mol. Pin1 inhibitors. Structural modifications designed to improve cell permeability resulted in Pin1 inhibitors with low micromolar anti-proliferative activities against cancer cells.

Bioorganic & Medicinal Chemistry Letters published new progress about 51656-68-9. 51656-68-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene, name is 3-(2,6-Dichlorophenyl)propanoic acid, and the molecular formula is C9H8Cl2O2, Application In Synthesis of 51656-68-9.

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

Shen, Hui published the artcileSynthesis of 3-substituted 2-oxindoles from secondary α-bromo-propionanilides via palladium-catalyzed intramolecular cyclization, Name: 3-(2,6-Dichlorophenyl)propanoic acid, the publication is Organic & Biomolecular Chemistry (2022), 20(17), 3589-3597, database is CAplus and MEDLINE.

A palladium-catalyzed intramol. cyclization of α-bromo-propionanilides was developed, delivering a series of 3-substituted 2-oxindoles in high yields. The method features easy to prepare starting materials, broad substrate scope and excellent functional group tolerance. A detailed mechanistic investigation was performed.

Organic & Biomolecular Chemistry published new progress about 51656-68-9. 51656-68-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene, name is 3-(2,6-Dichlorophenyl)propanoic acid, and the molecular formula is C10H10O2, Name: 3-(2,6-Dichlorophenyl)propanoic acid.

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

Russo Spena, Concetta published the artcileLiposomal delivery of a Pin1 inhibitor complexed with cyclodextrins as new therapy for high-grade serous ovarian cancer, Formula: C9H8Cl2O2, the publication is Journal of Controlled Release (2018), 1-10, database is CAplus and MEDLINE.

Pin1, a prolyl isomerase that sustains tumor progression, is overexpressed in different types of malignancies. Functional inactivation of Pin1 restrains tumor growth and leaves normal cells unaffected making it an ideal pharmaceutical target. Although many studies on Pin1 have focused on malignancies that are influenced by sex hormones, studies in ovarian cancer have lagged behind. Here, we show that Pin1 is an important therapeutic target in high-grade serous epithelial ovarian cancer. Knock down of Pin1 in ovarian cancer cell lines induces apoptosis and restrains tumor growth in a syngeneic mouse model. Since specific and non-covalent Pin1 inhibitors are still limited, the first liposomal formulation of a Pin1 inhibitor was designed. The drug was efficiently encapsulated in modified cyclodextrins and remotely loaded into pegylated liposomes. This liposomal formulation accumulates preferentially in the tumor and has a desirable pharmacokinetic profile. The liposomal inhibitor was able to alter Pin1 cancer driving-pathways trough the induction of proteasome-dependent degradation of Pin1 and was found to be effective in curbing ovarian tumor growth in vivo.

Journal of Controlled Release published new progress about 51656-68-9. 51656-68-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene, name is 3-(2,6-Dichlorophenyl)propanoic acid, and the molecular formula is C9H8Cl2O2, Formula: C9H8Cl2O2.

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

Chen, Liu published the artcileDesign and optimization of purine derivatives as in vivo active PDE10A inhibitors, Application In Synthesis of 51656-68-9, the publication is Bioorganic & Medicinal Chemistry (2017), 25(13), 3315-3329, database is CAplus and MEDLINE.

Phosphodiesterases are important enzymes regulating signal transduction mediated by second messenger mols. cAMP or cGMP. PDE10A is a unique member in the PDE family because of its selective expression in medium spiny neurons. It is recognized as anti-psychotic drug target. Based on the structural similarity between our previous chem. work on 8-aminoimidazo[1,2-a]pyrazines and the PDE10A inhibitors reported by Bartolome-Nebreda et al., we initialized a project for developing PDE10A inhibitors. After several rounds of optimization, we were able to obtain a few compounds with good PDE10A enzymic activity. And after further PDE enzymic selectivity study, metabolic stability assay and in vivo pharmacol. tests we identified two inhibitors as interesting lead compounds with the potential for further PDE10A lead optimization.

Bioorganic & Medicinal Chemistry published new progress about 51656-68-9. 51656-68-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene, name is 3-(2,6-Dichlorophenyl)propanoic acid, and the molecular formula is C9H8Cl2O2, Application In Synthesis of 51656-68-9.

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