Month: February 2023

Discovery of novel Akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells was written by Yu, Meng;Zeng, Minghui;Pan, Zhaoping;Wu, Fengbo;Guo, Li;He, Gu. And the article was included in European Journal of Medicinal Chemistry in 2020.Application of 587-88-2 This article mentions the following:

A series of thieno[2,3-d]pyrimidine derivatives I (X = O, CH₂, NR¹, Z = CH₂; X = CH₂, Z = nothing; R¹ = Me, cyclopropyl, PhCH₂, Me₂NCO, etc.; R² = 4-BrC₆H₄, 4-MeC₆H₄, 2-ClC₆H₄, etc.; R³ = Et, i-Pr, cyclohexyl, etc.) were designed, synthesized and evaluated as novel AKT1 inhibitors. In vitro antitumor assay results showed that compounds I (X = CH₂; Z = nothing; R² = 4-ClC₆H₄; R³ = Et, n-Bu, cyclopentyl, cyclohexyl) and I (X = CH₂; Z = nothing; R² = 4-BrC₆H₄; R³ = i-Pr) potently suppressed the enzymic activities of AKT1 and inhibited the proliferation of HepG2, Hep3B, Huh-7 and SMMC-7721 cancer cell lines. Among these derivatives, the compound I [X = CH₂; Z = nothing; R² = 4-ClC₆H₄; R³ = cyclopentyl; (II)] demonstrated the best inhibitory activities on AKT1 (IC₅₀ = 0.034娓璏) and Huh-7 cell (IC₅₀ = 0.076娓璏). A panel of biol. assays showed that compound II suppressed the cellular proliferation of Huh-7 through Akt/mTOR signaling pathway mediated autophagy mechanism. Furthermore, the antitumor capacity of II was validated in the s.c. Huh-7 xenograft models. Together, these results demonstrated that a novel small-mol. Akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma, which may afforded a potential drug candidate for targeted cancer therapy. In the experiment, the researchers used many compounds, for example, Ethyl 2-(4-fluorophenyl)acetate (cas: 587-88-2Application of 587-88-2).

Ethyl 2-(4-fluorophenyl)acetate (cas: 587-88-2) belongs to esters. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits. Acyl chlorides and acid anhydrides alcoholysis is another way to produce esters. Acyl chlorides and acid anhydrides react with alcohols to produce esters. Anydrous conditions are recommended since both acyl chlorides and acid anhydrides react with water.Application of 587-88-2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

The symbiotic bacteria Alcaligenes faecalis of the entomopathogenic nematodes Oscheius spp. exhibit potential biocontrol of plant- and entomopathogenic fungi was written by Shan, Shaojie;Wang, Wenwu;Song, Chunxu;Wang, Minggang;Sun, Bingjiao;Li, Yang;Fu, Yaqi;Gu, Xinghui;Ruan, Weibin;Rasmann, Sergio. And the article was included in Microbial Biotechnology in 2019.Name: Isopentyl 3-methylbutanoate This article mentions the following:

Soil-dwelling entomopathogenic nematodes (EPNs) kill arthropod hosts by injecting their symbiotic bacteria into the host hemolymph and feed on the bacteria and the tissue of the dying host for several generations cycles until the arthropod cadaver is completely depleted. The EPN-bacteria-arthropod cadaver complex represents a rich energy source for the surrounding opportunistic soil fungal biota and other competitors. We hypothesized that EPNs need to protect their food source until depletion and that the EPN symbiotic bacteria produce volatile and non-volatile exudations that deter different soil fungal groups in the soil. We isolated the symbiotic bacteria species (Alcaligenes faecalis) from the EPN Oscheius spp. and ran infectivity bioassays against entomopathogenic fungi (EPF) as well as against plant pathogenic fungi (PPF). We found that both volatile and non-volatile symbiotic bacterial exudations had neg. effects on both EPF and PPF. Such deterrent function on functionally different fungal strains suggests a common mode of action of A. faecalis bacterial exudates, which has the potential to influence the structure of soil microbial communities, and could be integrated into pest management programs for increasing crop protection against fungal pathogens. In the experiment, the researchers used many compounds, for example, Isopentyl 3-methylbutanoate (cas: 659-70-1Name: Isopentyl 3-methylbutanoate).

Isopentyl 3-methylbutanoate (cas: 659-70-1) belongs to esters. Carboxylic acid esters of low molecular weight are colourless, volatile liquids with pleasant odours, slightly soluble in water. Cyclic esters are called lactones, regardless of whether they are derived from an organic or inorganic acid. One example of an organic lactone is 绾?valerolactone.Name: Isopentyl 3-methylbutanoate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

UV synthesis PPMM – g – HEMA membrane and characterization was written by Huang, Lei;Yang, Li;Zheng, Lei;Shen, Weicheng. And the article was included in Shandong Huagong in 2016.Application In Synthesis of Benzyl benzodithioate This article mentions the following:

In this paper, using ferric chloride (FeCl₃) and benzophenone (BP) as co – photoinitiators, benzyl benzodithioate as chain transfer agent, the UV – induced graft polymerization of hydrophilic 2 – hydroxyethyl methacrylate (HEMA) onto hydrophobic polypropylene microporous membrane ( PPMM) was studied. Influencing factors of synthetic membranes were explored. Furthermore the poly (HEMA) – modified membrane surfaces were characterized by attenuated total reflectance Fourier transform IR spectroscopy . In the experiment, the researchers used many compounds, for example, Benzyl benzodithioate (cas: 27249-90-7Application In Synthesis of Benzyl benzodithioate).

Benzyl benzodithioate (cas: 27249-90-7) belongs to esters. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits. Many esters have the potential for conformational isomerism, but they tend to adopt an s-cis (or Z) conformation rather than the s-trans (or E) alternative, due to a combination of hyperconjugation and dipole minimization effects. The preference for the Z conformation is influenced by the nature of the substituents and solvent, if present. Lactones with small rings are restricted to the s-trans (i.e. E) conformation due to their cyclic structure.Application In Synthesis of Benzyl benzodithioate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Identification of novel compounds in rose absolute with gas chromatography/high-resolution mass spectrometry was written by Remy, Pierre-Alain;Sarrazin, Elise;Peres, Christophe;Dugay, Jose;David, Nathalie;Vial, Jerome. And the article was included in Flavour and Fragrance Journal in 2022.Synthetic Route of C12H20O2 This article mentions the following:

Gas Chromatog./High-Resolution Mass Spectrometry (HRMS) was used to identify new compounds in Rosa damascena and Rosa centifolia absolutes. These compounds were esters derived from the main alcs. of rose absolute (phenylethyl alc., geraniol, citronellol, nerol, and (E,E)-farnesol). Based on low-resolution mass spectrometry (LRMS) and HRMS data of rose absolutes, hypotheses were first formulated. In a second stage, the standards of these candidate structures were synthesized and analyzed by LRMS using apolar and polar columns. LRMS spectra of these standards, and apolar and polar retention indexes (RI) were compared with those of candidate structures. Only four out of nineteen mols. were validated by these three criteria mostly due to an important difference of polar RIs between the standards and the compounds detected in rose absolutes. In a third stage, absolutes were spiked with synthesized standards and were analyzed by HRMS on both apolar and polar columns to confirm the presence of these candidate structures. Finally, 19 new compounds were identified in Rosa damascena and Rosa centifolia absolutes. In the experiment, the researchers used many compounds, for example, (E)-3,7-Dimethylocta-2,6-dien-1-yl acetate (cas: 105-87-3Synthetic Route of C12H20O2).

(E)-3,7-Dimethylocta-2,6-dien-1-yl acetate (cas: 105-87-3) belongs to esters. Carboxylic acid esters of low molecular weight are colourless, volatile liquids with pleasant odours, slightly soluble in water. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.Synthetic Route of C12H20O2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Applicability of pea ingredients in baked products: Links between formulation, reactivity potential and physicochemical properties was written by Krause, Svenja;Asamoah, Eugenia Ayebea;Huc-Mathis, Delphine;Moulin, Gabrielle;Jakobi, Ralf;Rega, Barbara;Bonazzi, Catherine. And the article was included in Food Chemistry in 2022.Application In Synthesis of 5-Ethyldihydrofuran-2(3H)-one This article mentions the following:

This study aimed to evaluate the applicability of purified pea ingredients (starch and protein isolate) by assessing their potential to form volatile compounds during the different steps of sponge cake development compared to pea flour and wheat flour. While pea flour was highly susceptible to lipid oxidation during batter beating, the combination of purified pea starch and pea protein yielded significantly fewer oxidation markers with known green-beany off-odors. This was due more to the inactivation of lipoxygenase during flour fractionation than to differences in batter structure. However, fractionated ingredients were highly prone to participating in the Maillard reaction and caramelization during baking, leading to a more complex mixture of pyrazines, Strecker aldehydes and furanic compounds with potential malty and roasted notes compared to cakes based on pea flour or wheat flour. These findings confirm that using purified pea fractions can create high-quality products with an attractive composition In the experiment, the researchers used many compounds, for example, 5-Ethyldihydrofuran-2(3H)-one (cas: 695-06-7Application In Synthesis of 5-Ethyldihydrofuran-2(3H)-one).

5-Ethyldihydrofuran-2(3H)-one (cas: 695-06-7) belongs to esters. Esters are also usually derived from carboxylic acids. It may also be obtained by reaction of acid anhydride or acid halides with alcohols or by the reaction of salts of carboxylic acids with alkyl halides. Acyl chlorides and acid anhydrides alcoholysis is another way to produce esters. Acyl chlorides and acid anhydrides react with alcohols to produce esters. Anydrous conditions are recommended since both acyl chlorides and acid anhydrides react with water.Application In Synthesis of 5-Ethyldihydrofuran-2(3H)-one

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Synthesis of rac-bisabola-3(15),10-dien-7-ol was written by Weyerstahl, Peter;Schlicht, Volker. And the article was included in Liebigs Annalen/Recueil in 1997.Recommanded Product: Ethyl 4-methylenecyclohexanecarboxylate This article mentions the following:

1-Acetyl-4-methylenecyclohexane was obtained from 4-methylenecyclohexanecarboxylate, by DIBAH reduction, Grignard reaction, and oxidation A further Grignard reaction furnished rac-bisabola-3(15),10-dien-7-ol, which was isolated recently from vetiver oil. Its odor is mainly aldehydic (fatty, floral). In the experiment, the researchers used many compounds, for example, Ethyl 4-methylenecyclohexanecarboxylate (cas: 145576-28-9Recommanded Product: Ethyl 4-methylenecyclohexanecarboxylate).

Ethyl 4-methylenecyclohexanecarboxylate (cas: 145576-28-9) belongs to esters. Volatile esters with characteristic odours are used in synthetic flavours, perfumes, and cosmetics. Certain volatile esters are used as solvents for lacquers, paints, and varnishes. Acyl chlorides and acid anhydrides alcoholysis is another way to produce esters. Acyl chlorides and acid anhydrides react with alcohols to produce esters. Anydrous conditions are recommended since both acyl chlorides and acid anhydrides react with water.Recommanded Product: Ethyl 4-methylenecyclohexanecarboxylate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Chemical Composition of the Unexplored Volatile Fraction of Betula glandulosa, a Prevalent Shrub in Nunavik, Quebec was written by Seguin, Jean-Christophe;Fernandez, Xavier;Boudreau, Stephane;Voyer, Normand. And the article was included in Chemistry & Biodiversity in 2022.Recommanded Product: 118-61-6 This article mentions the following:

The volatile fraction of the leaves of Betula glandulosaICHX. has been investigated for its secondary metabolite composition by GC/MS and GC/FID. The rapid expansion of this shrub species in subarctic landscapes, like the ones found in Nunavik (Northern Quebec, Canada), highly impacts ecosystem dynamics. Yet, despite its abundance, few phytochem. investigations have yet been conducted on this species. In this study, we present the first phytochem. investigation of the volatile metabolites of B. glandulosa leaves. Although no essential oil was isolated, volatile compounds were extracted from the hydrosol by steam distillation The main metabolites observed were linalool (14.6-19.0 %), C6 oxylipins (known as green leaf volatiles, GLV; total of 18.2-40.2 %), eugenol (1.6-8.6 %) and 浼?terpineol (3.3-4.8 %). Dwarf birch is an important food source for insects and herbivores, so knowledge of its metabolite composition could help understand parts of its functional role in subarctic ecosystems. The composition of the volatile fraction could serve as marker for differentiating B. glandulosa from other dwarf birch species like Betula nana L. In the experiment, the researchers used many compounds, for example, Ethyl 2-hydroxybenzoate (cas: 118-61-6Recommanded Product: 118-61-6).

Ethyl 2-hydroxybenzoate (cas: 118-61-6) belongs to esters. Volatile esters with characteristic odours are used in synthetic flavours, perfumes, and cosmetics. Certain volatile esters are used as solvents for lacquers, paints, and varnishes. Cyclic esters are called lactones, regardless of whether they are derived from an organic or inorganic acid. One example of an organic lactone is 绾?valerolactone.Recommanded Product: 118-61-6

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Synthesis and calpain inhibitory activity of 浼?ketoamides with 2,3-methanoleucine stereoisomers at the P₂ position was written by Donkor, Isaac O.;Zheng, Xiaozhang;Miller, Duane D.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2000.Related Products of 87694-53-9 This article mentions the following:

A series of novel ketoamides I, (Ph = phenyl) incorporating all four 2,3-methanoleucine stereoisomers at the P₂ position, was synthesized. The compounds displayed a wide variation in K_i values for inhibition of calpain I depending on the configuration of the P₂ methanoleucine residue. However, similar variation in cathepsin B inhibition was not observed suggesting that the S₂ pocket of calpain I is more stereosensitive than that of cathepsin B. In the experiment, the researchers used many compounds, for example, (S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate (cas: 87694-53-9Related Products of 87694-53-9).

(S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate (cas: 87694-53-9) belongs to esters. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits, including apples, durians, pears, bananas, pineapples, and strawberries. Because of their lack of hydrogen-bond-donating ability, esters do not self-associate. Consequently, esters are more volatile than carboxylic acids of similar molecular weight.Related Products of 87694-53-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Quantitative analysis of Phthalate Esters by in-situ thermal desorption atmospheric pressure photoionization mass spectrometry using a dopant as the internal standard was written by Wang, Weimin;Jiang, Dandan;Jin, Liuyu;Wang, Pingping;Xu, Fuxing;Li, Haiyang;Ding, Chuan-Fan. And the article was included in International Journal of Mass Spectrometry in 2022.Formula: C20H26O4 This article mentions the following:

Phthalate Esters (PAEs) are a group of chems. widely used in plastic products, and they are also known as endocrine disruptors that can adversely affect the hormonal balance in humans. Since many food-contacting items, such as lunch boxes, fresh keeping film, disposable cups, are made of plastic, the PAEs can easily enter the human body through the polluted foods or drinks. Traditional anal. techniques involve laborious sample pretreatment and low-throughput anal., so it is necessary to develop techniques that can rapidly and quant. detect these compounds In this article, a miniaturized ion trap mass spectrometer (ITMS) was established firstly, then, an in-situ thermal desorption atm. pressure photoionization (in-situ TD-APPI) was designed, and the dopant was explored using for improving the sensitivity and as internal standard (IS) simultaneously in the anal. process. The in-situ TD-APPI presents good performance: (1) More than 20 times improvement in sensitivity compared with Nano-ESI for PAEs; (2) 12 kinds of phthalates were quantified with using acetone as the IS, and the LODs and LOQs ranges were found to be 0.02-1 娓璯/mL and 0.02-100 娓璯/mL, resp. The technique was also applied to the quantification of mixed solutions, and the results were validated by LC/MS. Finally, six categories of food-contacting items containing PAEs were analyzed with superficial content (ng/cm²) ranging from 0 to 6.20 ng/cm². These results demonstrate the potential of rapid quantification of anal. of PAEs in practical plastic food-contacting items by in-situ TD-APPI. In the experiment, the researchers used many compounds, for example, Dicyclohexyl phthalate (cas: 84-61-7Formula: C20H26O4).

Dicyclohexyl phthalate (cas: 84-61-7) belongs to esters. Esters are also usually derived from carboxylic acids. It may also be obtained by reaction of acid anhydride or acid halides with alcohols or by the reaction of salts of carboxylic acids with alkyl halides. Esters are more polar than ethers but less polar than alcohols. They participate in hydrogen bonds as hydrogen-bond acceptors, but cannot act as hydrogen-bond donors, unlike their parent alcohols. This ability to participate in hydrogen bonding confers some water-solubility.Formula: C20H26O4

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Glycan targeted polymeric antibiotic prodrugs for alveolar macrophage infections was written by Chen, Jasmin;Su, Fang-Yi;Das, Debobrato;Srinivasan, Selvi;Son, Hye-Nam;Lee, Brian;Radella, Frank II;Whittington, Dale;Monroe-Jones, Taylor;West, T. Eoin;Convertine, Anthony J.;Skerrett, Shawn J.;Stayton, Patrick S.;Ratner, Daniel M.. And the article was included in Biomaterials in 2019.Reference of 4163-60-4 This article mentions the following:

Alveolar macrophages resident in the lung are prominent phagocytic effector cells of the pulmonary innate immune response, and paradoxically, are attractive harbors for pathogens. Consequently, facultative intracellular bacteria, such as Francisella tularensis, can cause severe systemic disease and sepsis, with high morbidity and mortality associated with pulmonary infection. Current clin. treatment, which involves exhaustive oral or i.v. antibiotic therapy, has limitations such as systemic toxicity and off-target effects. Pulmonary administration represents a promising alternative to systemic dosing for delivering antibiotics directly to the lung. Here, we present synthesized mannosylated ciprofloxacin polymeric prodrugs for efficient pulmonary delivery, targeting, and subsequent internalization by alveolar macrophages. We demonstrate significant improvement in efficacy against intracellular infections in an otherwise uniformly lethal airborne Francisella murine model (F. novicida). When administered to the lungs of mice in a prophylactic regimen, the mannosylated ciprofloxacin polymeric prodrugs led to 50% survival. In a treatment regimen that was concurrent with infection, the survival of mice increased to 87.5%. Free ciprofloxacin antibiotic was ineffective in both cases. This significant difference in antibacterial efficacy demonstrates the impact of this delivery platform based on improved physiochem., pharmacokinetic, and pharmacodynamic properties of ciprofloxacin administered via our glycan polymeric prodrug. This modular platform provides a route for overcoming the limitations of free drug and increasing efficacy in treatment of intracellular infection. In the experiment, the researchers used many compounds, for example, (2S,3R,4S,5S,6R)-6-(Acetoxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetrayl tetraacetate (cas: 4163-60-4Reference of 4163-60-4).

(2S,3R,4S,5S,6R)-6-(Acetoxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetrayl tetraacetate (cas: 4163-60-4) belongs to esters. Carboxylic acid esters of low molecular weight are colourless, volatile liquids with pleasant odours, slightly soluble in water. Esters are more polar than ethers but less polar than alcohols. They participate in hydrogen bonds as hydrogen-bond acceptors, but cannot act as hydrogen-bond donors, unlike their parent alcohols. This ability to participate in hydrogen bonding confers some water-solubility.Reference of 4163-60-4

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics