Month: December 2022

Shen, Jincheng published the artcileIntegrated metabolomic and transcriptomic analysis reveals factors underlying differences in fruit quality between Fragaria nilgerrensis and Fragaria pentaphylla, COA of Formula: C6H6N2O, the publication is Journal of the Science of Food and Agriculture (2022), 102(8), 3287-3296, database is CAplus and MEDLINE.

Strawberries have become one of the most popular fruits because of their unique flavor and high nutritional value. Fruit quality and price are the most important criteria that determine consumer acceptability. Fragaria nilgerrensis and Fragaria pentaphylla are two wild Asian diploid strawberry species that differ in fruit color, taste, and aroma. To understand the mol. mechanisms involved in the formation of high-quality strawberry fruit, we integrated transcriptomics and metabolomics research methods to compare the metabolic and biosynthetic mechanisms of the two Fragaria species. F. nilgerrensis fruit has higher amino acid and lipid contents and a higher sugar-to-acid ratio than F. pentaphylla fruit does, underlying their superior nutritional value, aroma, firmness, and taste. Compared with F. nilgerrensis fruit, F. pentaphylla fruit contained more flavonoids, indicating its enhanced color and health benefits. In addition, candidate structural genes that regulate the biosynthesis of flavonoids, amino acids, and glycerophospholipids in the two strawberry fruit were screened. The differences in aroma, firmness, and taste between F. nilgerrensis fruit and F. pentaphylla fruit are probably due to differences in their amino acid and lipid contents, as well as the difference in their sugar-to-acid ratios. Eight key structural genes that may play important roles in the biosynthesis of amino acids, lipids, and flavonoids were identified. 2021 Society of Chem. Industry.

Journal of the Science of Food and Agriculture published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C15H14BNO4S, COA of Formula: C6H6N2O.

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

Wang, Aimin published the artcileThymidine Kinase 1 Mediates the Synergistic Antitumor Activity of Ubenimex and Celecoxib via Regulation of Cell Cycle in Colorectal Cancer., COA of Formula: C17H14F3N3O2S, the publication is The Journal of pharmacology and experimental therapeutics (2022), 382(2), 188-198, database is MEDLINE.

Colorectal cancer (CRC) is a common clinical malignant tumor of the digestive system that seriously affects the health and life of patients. Because it is difficult to cure CRC, the strategy of drug combination is often used in clinical therapy. This study mainly revealed that ubenimex and/or celecoxib exerted anti-colon cancer effects in vitro and in vivo, and the efficacy was significantly enhanced when the two drugs were combined. The combination of the two drugs induced significantly stronger cell-cycle arrest than did the single drug, and also enhanced the antitumor efficacy of 5-fluorouracil and its derivatives. At the same time, the expression of thymidine kinase 1 (TK1) protein was decreased through regulating the level of TK1 mRNA treated with celecoxib and/or ubenimex, but the combination drugs exhibited much more reduction of TK1 mRNA and protein as compared with the single agent alone. TK1 may be the molecular target of the combination of two drugs to exert the anti-colorectal cancer effect. In summary, this research demonstrates that celecoxib combined with ubenimex inhibits the development of colorectal cancer in vitro and in vivo, making them a viable combination regimen. SIGNIFICANCE STATEMENT: In this study, our data reveal the great potential of celecoxib combined with ubenimex in the treatment of colorectal cancer, providing new ideas for clinical antitumor drug regimens and theoretical reference for drug development.

The Journal of pharmacology and experimental therapeutics published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C13H14N2O, COA of Formula: C17H14F3N3O2S.

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

Shoair, Abdel Ghany F. published the artcileElectrochemical and catalytic properties of oxo-ruthenate(VI) in aqueous alkaline medium, HPLC of Formula: 1453-82-3, the publication is International Journal of Electrochemical Science (2021), 16(5), 210545, database is CAplus.

The complex K₂[Ru^(III)Cl₅(H₂O)] has been prepared and characterized by different spectroscopic techniques (IR and UV-VIS). The electrochem. properties of this complex were investigated at different pH′s using Robinson buffer solutions The cyclic voltammograms exhibited three redox different oxidation and potential peaks due to generation of Ru(III), Ru(IV), Ru(V) and Ru(VI) ions. The catalytic activity of K₂[Ru^(III)Cl₅(H₂O)] towards the hydration of some aromatic and three heterocyclic nitriles to their corresponding amides was investigated with excess of three co-oxidants K₂S₂O₈, NaOCl and KBrO₃. A number of factors have been investigated and the best yields were obtained with K₂S₂O₈ as a co-oxidant in a 1.0 M KOH at 80 °C. Both spectroscopic and electrochem. techniques were used to establish the nature of active species in this catalytic reaction and the active catalyst was found to be K₂[Ru^(VI)O₃(OH)₂], as well as to explain the possible reaction mechanism. The suggested mechanism included the coordination of nitrile to ruthenium center followed by liberation of the corresponding amide and the active complex again.

International Journal of Electrochemical Science published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C9H5ClO2, HPLC of Formula: 1453-82-3.

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

Kempf, Dale J. published the artcileDiscovery of Ritonavir, a Potent Inhibitor of HIV Protease with High Oral Bioavailability and Clinical Efficacy, HPLC of Formula: 14294-10-1, the publication is Journal of Medicinal Chemistry (1998), 41(4), 602-617, database is CAplus and MEDLINE.

The structure-activity studies leading to the potent and clin. efficacious HIV protease inhibitor ritonavir are described. Beginning with the moderately potent and orally bioavailable inhibitor A-80987, systematic investigation of peripheral (P3 and P2′) heterocyclic groups designed to decrease the rate of hepatic metabolism provided analogs with improved pharmacokinetic properties after oral dosing in rats. Replacement of pyridyl groups with thiazoles provided increased chem. stability toward oxidation while maintaining sufficient aqueous solubility for oral absorption. Optimization of hydrophobic interactions with the HIV protease active site produced ritonavir, with excellent in vitro potency (EC₅₀ = 0.02 μM) and high and sustained plasma concentrations after oral administration in 4 species. Details of the discovery and preclin. development of ritonavir are described.

Journal of Medicinal Chemistry published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C5H10N2OS, HPLC of Formula: 14294-10-1.

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

Bridge, Thomas published the artcileSite-Specific Encoding of Photoactivity in Antibodies Enables Light-Mediated Antibody-Antigen Binding on Live Cells, Quality Control of 2418-95-3, the publication is Angewandte Chemie, International Edition (2019), 58(50), 17986-17993, database is CAplus and MEDLINE.

Antibodies found applications in several fields, including, medicine, diagnostics, and nanotechnol., yet methods to modulate antibody-antigen binding using an external agent remain limited. Here, the authors have developed photoactive antibody fragments by genetic site-specific replacement of single tyrosine residues with photocaged tyrosine, in an antibody fragment, 7D12. A simple and robust assay is adopted to evaluate the light-mediated binding of 7D12 mutants to its target, epidermal growth factor receptor (EGFR), on the surface of cancer cells. Presence of photocaged tyrosine reduces 7D12-EGFR binding affinity by over 20-fold in two out of three 7D12 mutants studied, and binding is restored upon exposure to 365 nm light. Mol. dynamics simulations explain the difference in effect of photocaging on 7D12-EGFR interaction among the mutants. Finally, the authors demonstrate the application of photoactive antibodies in delivering fluorophores to EGFR-pos. live cancer cells in a light-dependent manner.

Angewandte Chemie, International Edition published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Quality Control of 2418-95-3.

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

Saniee, Fateme published the artcileGlutamate-urea-based PSMA-targeted PLGA nanoparticles for prostate cancer delivery of docetaxel, Synthetic Route of 2418-95-3, the publication is Pharmaceutical Development and Technology (2021), 26(4), 381-389, database is CAplus and MEDLINE.

Targeted drug delivery is a tool to make treatment more specific, selective, and effective and to prevent unwanted complications. Prostate specific membrane antigen (PSMA) is a useful biomarker in order to monitor and control prostate cancer. Glutamate-Urea-R (Glu-Urea-R) is a PSMA enzyme inhibitor capable of binding to this surface marker of prostate cancer cell in an efficient and special manner. The aim of this project was to develop a docetaxel-loaded nanoparticle of poly (lactic-co-glycolic acid) polyethylene glycol which is cojugated to a urea-based anti-PSMA ligand named glutamate-urea-lysine (glu-urea-lys) for targeted delivery of docetaxel in prostate cancer. The obtained nanoparticles, prepared by nanopptn. method, were spheres with a particle size of around 150 nm and zeta potential of -7.08 mV. Uptake studies on the PC3 (as PSMA neg.) and LNCaP (as PSMA pos.) cells demonstrated that drug uptake was efficient by the PSMA pos. cells. IC₅₀ of targeted NPs on LNCaP cell line compared to non-targeted ones was reduced by more than 70% in three different incubation times of 24, 48, and 72 h. In conclusion, the nanoparticles are expected to specifically transport docetaxel to PSMA-pos. prostate cancer cells and consequently, enhance the antitumor efficacy of docetaxel on these cells.

Pharmaceutical Development and Technology published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Synthetic Route of 2418-95-3.

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

Liu, Fangyao published the artcileControlled radical polymerization of N-acryloylglycinamide and UCST-type phase transition of the polymers, Name: N-(2-Amino-2-oxoethyl)acrylamide, the publication is Journal of Polymer Science, Part A: Polymer Chemistry (2012), 50(23), 4920-4928, database is CAplus.

N-Acryloylglycinamide was polymerized via the reversible addition fragmentation transfer process without sacrificing its key property, the upper critical solution temperature in water. This could be achieved by choosing an appropriate nonionic initiator [2,2′-azobis(4-methoxy-2.4-dimethyl valeronitrile) (V-70)] and nonionic chain-transfer agent (cyanomethyl dodecyl trithiocarbonate). A good molar mass control was accomplished as proved by the linear increase of molar mass with conversion, a chain extension experiment, and low dispersity. The influence of molar mass, polymer end groups, or salt concentration on the cloud point was analyzed by turbidimetry. Polymer end groups exerted a distinct effect on the cloud points, whereas the influence increased with decreasing molar masses. © 2012 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem, 2012.

Journal of Polymer Science, Part A: Polymer Chemistry published new progress about 2479-62-1. 2479-62-1 belongs to amides-buliding-blocks, auxiliary class Monomers,Acrylamide Monomers, name is N-(2-Amino-2-oxoethyl)acrylamide, and the molecular formula is C5H8N2O2, Name: N-(2-Amino-2-oxoethyl)acrylamide.

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

Liu, Fangyao published the artcileA Non-ionic Thermophilic Hydrogel with Positive Thermosensitivity in Water and Electrolyte Solution, Formula: C5H8N2O2, the publication is Macromolecular Chemistry and Physics (2014), 215(15), 1466-1472, database is CAplus.

The first example of a chem. crosslinked synthetic non-ionic hydrogel showing reversible pos. swelling behavior in pure water as well as electrolyte solution is highlighted. Homopolymeric hydrogels are synthesized from N-acryloylglycinamide with N,N’-methylenbis(acrylamide) as a chem. crosslinker via free radical polymerization in DMSO. The swelling-ratio dependency of the hydrogels upon temperature as well as on the amounts of crosslinker from 1 to 4.8 mol% is studied. With 1 mol% crosslinker, the hydrogel is able to take up over three times water of its weight at 37 °C in pure water and phosphate-buffered saline. All the samples show almost 100% of reversibility for at least 6 d up to 37 °C irresp. of the amount of the crosslinker, making them promising candidates for biomedical applications. The sample with a higher amount of crosslinker, i.e., 4.8 mol% is even stable for over 6 d at 70 °C.

Macromolecular Chemistry and Physics published new progress about 2479-62-1. 2479-62-1 belongs to amides-buliding-blocks, auxiliary class Monomers,Acrylamide Monomers, name is N-(2-Amino-2-oxoethyl)acrylamide, and the molecular formula is C5H8N2O2, Formula: C5H8N2O2.

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

Liu, Fangyao published the artcileAtom transfer radical polymerization as a tool for making poly(N-acryloylglycinamide) with molar mass independent UCST-type transitions in water and electrolytes, Category: amides-buliding-blocks, the publication is Polymer Chemistry (2013), 4(10), 3123-3131, database is CAplus.

Atom transfer radical polymerization (ATRP) of N-acryloylglycinamide has been used as a tool to make poly(NAGA) showing UCST-type phase transitions in water and electrolytes independent of molar mass and end-groups. We hypothesized that similarity in the structure of polymer chain ends with the repeat unit of poly(NAGA) could help in eliminating the effect of molar mass dependence of the cloud point especially in the low molar mass region. The monomer-like end-groups were introduced by choosing an appropriate initiator for ATRP like chloropropionamide (CPA). The catalyst system CuCl/CuCl₂ and tris[2-(dimethylamino)ethyl]-amine (Me₆TREN) as a ligand provided controlled polymerization of NAGA in DMSO at 45° with UCST-type transitions retained in water and electrolytes without being influenced by chain ends/M mass and high concentration of salts like NaCl and Na₂SO₄.

Polymer Chemistry published new progress about 2479-62-1. 2479-62-1 belongs to amides-buliding-blocks, auxiliary class Monomers,Acrylamide Monomers, name is N-(2-Amino-2-oxoethyl)acrylamide, and the molecular formula is C5H8N2O2, Category: amides-buliding-blocks.

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

Moutaoukil, Zakaria published the artcileN-Alkylation of organonitrogen compounds catalyzed by methylene-linked bis-NHC half-sandwich ruthenium complexes, Synthetic Route of 1453-82-3, the publication is Organic & Biomolecular Chemistry (2022), 20(4), 831-839, database is CAplus and MEDLINE.

An efficient ruthenium-catalyzed N-alkylation of amines, amides and sulfonamides was developed employing novel pentamethylcyclopentadienylruthenium(II) complexes bearing the methylene linked bis(NHC) ligand bis(3-methylimidazol-2-ylidene)methane. The acetonitrile complex I was proved to be particularly effective with a broad range of substrates with low catalyst loading (0.1-2.5 mol%) and high functional group tolerance under mild conditions. A total of 52 N-alkylated organonitrogen compounds including biol. relevant scaffolds were synthesized from (hetero)aromatic and aliphatic amines, amides and sulfonamides using alcs. or diols as alkylating agents in up to 99% isolated yield, even on gram-scale reactions. In the case of sulfonamides, it was the first example of N-alkylation employing a transition-metal complex bearing NHC ligands.

Organic & Biomolecular Chemistry published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Synthetic Route of 1453-82-3.

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