Tag: M.W=250-300

Shiraishi, Takaya; Sakaitani, Masahiro; Otsuguro, Satoko; Maenaka, Katsumi; Suzuki, Toshiharu; Nakaya, Tadashi published the artcile< Novel Notch signaling inhibitor NSI-1 suppresses nuclear translocation of the Notch intracellular domain>, COA of Formula: C19H34O2, the main research area is novel notch signaling inhibitor NSI nuclear translocation intracellular domain.

The Notch receptor serves a fundamental role in the regulation of cell fate determination through intracellular signal transmission. Mutation of the Notch receptor results in abnormal active signaling, leading to the development of diseases involving abnormal cell growth, including malignant tumors. Therefore, the Notch signaling pathway is a useful pharmacol. target for the treatment of cancer. In the present study, a compound screening system was designed to identify inhibitors of the Notch signaling targeting Notch intracellular domain (NICD). A total of 9,600 compounds were analyzed using the Michigan Cancer Foundation-7 (MCF7) human breast adenocarcinoma cell line and the SH-SY5Y human neuroblastoma cell line with the reporter assay system using an artificial protein encoding a partial Notch carboxyl-terminal fragment fused to the Gal4 DNA-binding domain. The mol. mechanism underlying the inhibition of Notch signaling by a hit compound was further validated using biochem. and cell biol. approaches. Using the screening system, a potential candidate, Notch signaling inhibitor-1 (NSI-1), was isolated which showed 50% inhibition at 6.1μM in an exogenous Notch signaling system. In addition, NSI-1 suppressed the nuclear translocation of NICD and endogenous gene expression of hairy and enhancer of split-1, indicating that NSI-1 specifically targets Notch. Notably, NSI-1 suppressed the cell viability of MCF7 cells and another human breast adenocarcinoma cell line, MDA-MB-231 exhibiting constitutive and high Notch signaling activity, whereas no significant effect was observed in the SH-SY5Y cells bearing a lower Notch signaling activity. NSI-1 significantly suppressed the viability of SH-SY5Y cells expressing exogenous human Notch1. These results indicate that NSI-1 is a novel Notch signaling inhibitor and suggest its potential as a useful drug for the treatment of diseases induced by constitutively active Notch signaling.

International Journal of Molecular Medicine published new progress about Amino acids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, COA of Formula: C19H34O2.

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

Inoo, Akane; Fukutsuka, Tomokazu; Miyahara, Yuto; Kondo, Yasuyuki; Yokoyama, Yuko; Miyazaki, Kohei; Abe, Takeshi published the artcile< Molecular structural influence of glymes on Co-intercalation behavior of solvated Li+ in graphite electrodes>, Quality Control of 112-63-0, the main research area is tetraglyme lithium graphite composite electrode ionic conductivity.

Solvated Li+ ions are intercalated into graphite in a dilute glyme-based solution and this reaction has attracted much attention for use in advanced lithium-ion batteries due to their high rate capability. In this study, Li+ co-intercalation behaviors in asym. glymes (CH3O(CH2CH2O)nC4H9, n = 2 or 3) were investigated and compared to those in sym. glymes (CH3O(CH2CH2O)nCH3, n = 1-4). Despite the large alkyl sidechains of asym. glymes, co-intercalation reactions of solvated Li+ proceeded as well as those in sym. glymes. In charge and discharge measurements, the reversible capacities in asym. glyme-based solutions were smaller than those in sym. glymes except for tetraglyme, which showed the lowest reversible capacity. There was no clear difference in the sandwich distances of glyme-Li-GICs calculated from X-ray diffraction patterns of both sym. and asym. glymes. Therefore, solvated Li+ ions with asym. glymes occupied more space in the graphite interlayer compared to sym. glymes, which resulted in smaller reversible capacities for asym. glymes. These results demonstrate the influence of solvent-related structures of GICs on reversible capacities for co-intercalation systems.

Journal of the Electrochemical Society published new progress about Composites. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Quality Control of 112-63-0.

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

Li, Wanfang; Lu, Bin; Xie, Xiaomin; Zhang, Zhaoguo published the artcile< Ru-Catalyzed Chemo- and Enantioselective Hydrogenation of β-Diketones Assisted by the Neighboring Heteroatoms>, Synthetic Route of 112-63-0, the main research area is diketone beta hydrogenation chemo enantioselective ruthenium catalyst.

A highly chemo- and enantioselective hydrogenation of β-diketones was achieved by using [Ru(benzene)(S)-SunPhosCl]Cl for consistency in THF. The neighboring heteroatoms played important roles in guaranteeing the reactivity and controlling the chemoselectivity. These results suggested a potential approach for the clean and facile synthesis of functionalized chiral β-hydroxy ketones, which could otherwise be prepared through much less step-economic transformations.

Organic Letters published new progress about Diketones, 1,3-diketones Role: RCT (Reactant), RACT (Reactant or Reagent). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Synthetic Route of 112-63-0.

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

Pulvirenti, Luca; Monforte, Francesca; Lo Presti, Francesca; Li Volti, Giovanni; Carota, Giuseppe; Sinatra, Fulvia; Bongiorno, Corrado; Mannino, Giovanni; Cambria, Maria Teresa; Condorelli, Guglielmo Guido published the artcile< Synthesis of MIL-Modified Fe3O4 Magnetic Nanoparticles for Enhancing Uptake and Efficiency of Temozolomide in Glioblastoma Treatment>, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is enhancing Uptake Efficiency temozolomide Glioblastoma Treatment; Fe3O4; glioblastoma; magnetic nanoparticles; metal organic frameworks; temozolomide.

A nanometric hybrid system consisting of a Fe3O4 magnetic nanoparticles modified through the growth of Fe-based Metal-organic frameworks of the MIL (Materials Institute Lavoiser) was developed. The obtained system retains both the nanometer dimensions and the magnetic properties of the Fe3O4 nanoparticles and possesses increased the loading capability due to the highly porous Fe-MIL. It was tested to load, carry and release temozolomide (TMZ) for the treatment of glioblastoma multiforme one of the most aggressive and deadly human cancers. The chem. characterization of the hybrid system was performed through various complementary techniques: X-ray-diffraction, thermogravimetric anal., FT-IR and X-ray photoelectron spectroscopies. The nanomaterial showed low toxicity and an increased adsorption capacity compared to bare Fe3O4 magnetic nanoparticles (MNPs). It can load about 12 mg/g of TMZ and carry the drug into A172 cells without degradation Our exptl. data confirm that, after 48 h of treatment, the TMZ-loaded hybrid nanoparticles (15 and 20μg/mL) suppressed human glioblastoma cell viability much more effectively than the free drug. Finally, we found that the internalization of the MIL-modified system is more evident than bare MNPs at all the used concentrations both in the cytoplasm and in the nucleus suggesting that it can be capable of overcoming the blood-brain barrier and targeting brain tumors. In conclusion, these results indicate that this combined nanoparticle represents a highly promising drug delivery system for TMZ targeting into cancer cells.

International Journal of Molecular Sciences published new progress about Astrocytoma. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate.

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

Potikha, L. M.; Kovtunenko, V. A.; Kisil, V. M. published the artcile< Condensed isoquinolines. Part 21. Condensation of o-bromomethylphenylacetonitrile with substituted anthranilic acids>, Formula: C19H34O2, the main research area is bromomethylbenzeneacetonitrile anthranilate cyclocondensation; isoquinoquinazolinone hydro preparation tautomerism.

The reaction of substituted anthranilic acids and esters with ortho-bromomethylphenylacetonitrile gives 2,3-disubstituted 7,12-dihydro-5H-isoquino[2,3-a]quinazolin-5-one hydrobromides. It was found that 7,12-dihydro-5H-isoquino[2,3-a]quinazolin-5-ones can exist in the two tautomeric imine and enamine forms. The tautomeric equilibrium position depends on the nature and position of the substituent in the quinazoline fragment. The borohydride reduction, oxidation, and reaction of the 7,12-dihydro-5H-isoquino[2,3-a]quinazolin-5-ones with electrophilic reagents was studied.

Chemistry of Heterocyclic Compounds (New York, NY, United States) published new progress about Aromatic amino acids Role: RCT (Reactant), RACT (Reactant or Reagent). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Formula: C19H34O2.

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

Liu, Chong; Sun, Dan; Zheng, Hong-Xiang; Wang, Guo-Bao; Liu, Wen-Shen; Cao, Yue; Tang, Ye-Tao; Qiu, Rong-Liang published the artcile< The limited exclusion and efficient translocation mediated by organic acids contribute to rare earth element hyperaccumulation in Phytolacca americana>, Reference of 112-63-0, the main research area is Phytolacca rare earth element translocation organic acid; Hyperaccumulator; Rhizosphere; Root exudate; Translocation; Yttrium.

Organic acids play an important role in metal tolerance, uptake, and translocation in hyperaccumulators. Phytolacca americana is a rare earth element (REE) hyperaccumulator, but the underlying mechanisms on REE tolerance and accumulation mediated by organic acids are poorly understood. Here, we reported for the first time the strategy of P. americana to enhance REE tolerance and accumulation through organic acids from root external secretion to internal biosynthesis. Different from the exclusion of heavy metal by organic acid in the typical plants, the results showed that oxalate secretion (0.3-0.6μmol h-1 g-1 root DW) induced by yttrium (Y) could not prevent Y from entering the roots, resulting in excess Y uptake by P. americana. Yttrium stress also stimulated the accumulation of malate and citrate by 1.4- and 2.0-folds in the root cortex. Exogenous malate and citrate promoted the redistribution of Y from the root cell walls to the shoot by 30% and 21%, resp. Based on comparative transcriptome anal., 6-fold up-regulation was observed in PaNIP1;2, whose homol. AtNIP1;2 is responsible for the transport of Al-malate in Arabidopsis. These results suggested that the promoted formation of Y-malate complexes within the roots potentially accelerated the transport of Y from P. americana roots to shoots through PaNIP1;2. Our study revealed the potential mechanism of organic acids in the external exclusion and internal detoxification and translocation of REE in P. americana roots, which provided a basis for improving the efficiency of REE phytoextraction

Science of the Total Environment published new progress about Arabidopsis. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Reference of 112-63-0.

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

Gnanadoss, Lalitha; Vijayalakshmi, A. published the artcile< Steric effects in oxidation of primary alcohols by pyridinium hydrobromide perbromide>, Related Products of 112-63-0, the main research area is steric effect oxidation alc; oxidation alc bromide kinetics; pyridinium hydrobromide perbromide oxidation alc; LFER oxidation alc bromide; isokinetic temperature oxidation alc.

Kinetics of oxidation of a homologous series of nine primary alcs. was studied in 60 volume% aqueous AcOH using pyridinium hydrobromide perbromide as the oxidizing agent. The results were interpreted in terms of steric effects and a plot of log rate vs. υ, the steric parameter introduced by M. Charton (1975) is linear. A mechanism involving steric relief in the rate-determining step is proposed.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Related Products of 112-63-0.

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

Chiu, George; Li, Shengjian; Connolly, Peter J.; Pulito, Virginia; Liu, Jingchun; Middleton, Steven A. published the artcile< (Arylpiperazinyl)cyclohexylsufonamides: Discovery of α1a/1d-selective adrenergic receptor antagonists for the treatment of Benign Prostatic Hyperplasia/Lower Urinary Tract Symptoms (BPH/LUTS)>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is arylpiperazinyl cyclohexylsufonamide derivative preparation adrenergic receptor antagonist prostatic hyperplasia.

Benign Prostatic Hyperplasia/Lower Urinary Tract Symptoms (BPH/LUTS) can be effectively treated by α1-adrenergic receptor antagonists. Unfortunately, all currently marketed α1 blockers produced CV related side effects that are caused by the subtype nonselective nature of the drugs. To overcome this problem, it was postulated that a α1a/1d subtype selective antagonist would bring more benefit for the treatment of BPH/LUTS. In developing selective α1a/1d ligands, (arylpiperazinyl)cyclohexylsulfonamides were synthesized and their binding profiles against three cloned human α1-adrenergic receptor subtypes were evaluated. Many compounds show equal affinity for both α1a and α1d subtypes with good selectivity against the α1b subtype. They also overcome the problem of dopamine receptor affinity that previous analogs had exhibited.

Bioorganic & Medicinal Chemistry Letters published new progress about Benign prostatic hyperplasia. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate.

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

Ledneczki, Istvan; Tapolcsanyi, Pal; Gabor, Eszter; Visegrady, Andras; Vass, Marton; Eles, Janos; Holm, Patrik; Horvath, Anita; Pocsai, Aniko; Maho, Sandor; Greiner, Istvan; Kramos, Balazs; Beni, Zoltan; Koti, Janos; Kancz, Anna E.; Than, Marta; Kolok, Sandor; Laszy, Judit; Balazs, Ottilia; Bugovits, Gyula; Nagy, Jozsef; Vastag, Monika; Szajli, Agota; Bozo, Eva; Levay, Gyorgy; Lendvai, Balazs; Nemethy, Zsolt published the artcile< Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach>, Application In Synthesis of 112-63-0, the main research area is pos allosteric modulator nicotinic acetylcholine receptor drug discovery; Cognitive improvement; Nicotinic alpha 7 receptor; Positive allosteric modulator; Scaffold hopping; Structure activity relationship.

The paper focuses on the scaffold hopping-based discovery and characterization of novel nicotinic alpha 7 receptor pos. modulator (α7 nAChR PAM) ligands around the reference mol. (A-867744). First, substantial efforts were carried out to assess the importance of the various pharmacophoric elements on the in vitro potency (SAR evaluation) by chem. modifications. Subsequently, several new derivatives with versatile, heteroaromatic central cores were synthesized and characterized. A promising, pyrazole-containing new chemotype with good physicochem. and in vitro parameters was identified. Retrospective anal. based on homol. modeling was also carried out. Besides its favorable in vitro characteristics, the most advanced derivative 69 also showed in vivo efficacy in a rodent model of cognition (scopolamine-induced amnesia in the mouse place recognition test) and acceptable pharmacokinetic properties. Based on the in vivo data, the resulting mol. with advanced drug-like characteristics has the possibility to improve cognitive performance in a biol. relevant dose range, further strengthening the view of the supportive role of α7 nACh receptors in the cognitive processes.

European Journal of Medicinal Chemistry published new progress about Acylation. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application In Synthesis of 112-63-0.

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

Hu, Jingyi; Huang, Hai; Che, Yuan; Ding, Chujie; Zhang, Lu; Wang, Yun; Hao, Haiping; Shen, Hong; Cao, Lijuan published the artcile< Qingchang Huashi Formula attenuates DSS-induced colitis in mice by restoring gut microbiota-metabolism homeostasis and goblet cell function>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is qingchang huashi formula colitis gut microbiota homeostasis; Goblet cell; Gut microbiota; Qingchang Huashi formula; Ulcerative colitis.

The aim of this study was to clearly define the effect of QHF and its components, Baitouweng (PBR) and Baizhi (ADR) on treating UC. Pharmacodynamic effects of QHF and single herb were evaluated in dextran sulfate sodium (DSS) induced acute or chronic colitis mice. The colorectal tissues were used to detect levels of IL-1β, IL-6 and TNF-α by ELISA or qRT-PCR. The expression of NLRP3, Caspase 1 and IL-1β were examined by western blotting. QHF significantly inhibited colitis, protected mice from the loss of body weight and colon shorten. We verified that while ADR was responsible for QHF s effect on maintaining gut microbiota homeostasis and metabolism, PBR was more prominent in keeping crypt stem cells proliferation and colonic goblet cells function. Moreover, we demonstrated that the alleviation of colitis by QHF was associated with the restoration of gut microbiota-metabolism homeostasis, protection of intestinal epithelial barrier and regulation of NLRP3/IL-1β pathway. The finding of the present study suggested that QHF is curative in DSS-induced colitis by restoring gut microbiota-metabolism homeostasis and goblet cells function. An optimized QHF was constituted by ADR and PBR, which showed comparable efficacy on colitis to that of QHF. Our work probed out the active constitutes as well as the relevant pharmacol. mechanisms of QHF, shedding light on potential new drug combination for the treatment of IBD.

Journal of Ethnopharmacology published new progress about Animal gene, IL1B Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate.

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