Category: 112-63-0

Buck, Jason R.; Saleh, Sam; Imam Uddin, Md.; Manning, H. Charles published the artcile< Rapid, microwave-assisted organic synthesis of selective V600EBRAF inhibitors for preclinical cancer research>, Electric Literature of 112-63-0, the main research area is azaindole PLX4720 PLX4032 preparation BRAF inhibitor microwave irradiation.

We report dramatically improved total syntheses of two highly selective V600EBRAF inhibitors, PLX4720 and PLX4032, that leverages microwave-assisted organic synthesis (MAOS). Compared with previously reported approaches, our novel MAOS method significantly reduces overall reaction time without compromising yield. In addition to providing a gram-scale route to these compounds for preclin. oncol. research, we anticipate this approach could accelerate the synthesis of azaindoles in high-throughput, library-based formats.

Tetrahedron Letters published new progress about Microwave irradiation. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Electric Literature of 112-63-0.

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

Wilson, Kenneth J.; Illig, Carl R.; Chen, Jinsheng; Wall, Mark J.; Ballentine, Shelley K.; Des Jarlais, Renee L.; Chen, Yanmin; Schubert, Carsten; Donatelli, Robert; Petrounia, Ioanna; Crysler, Carl S.; Molloy, Christopher J.; Chaikin, Margery A.; Manthey, Carl L.; Player, Mark R.; Tomczuk, Bruce E.; Meegalla, Sanath K. published the artcile< Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors>, Application of C19H34O2, the main research area is imidazolecarboxamide cyclohexenylaryl nitrile preparation ion channel activity FMS inhibitor.

A series of saturated and aromatic 4-heterocycles of reduced basicity I (R1 = Ph, 4-H2NC6H4, 2-pyridyl, 2,6-dioxo-4-piperidinyl, 2-oxo-3,4,5,6-tetrahydro-1H-pyrimidin-5-yl, etc.; R2 = H, Me) was prepared and evaluated in an attempt to improve the bioavailability of FMS kinase inhibitors and the cardiovascular safety profile over lead arylamide I (R1 = 4-piperidinyl; R2 = H), which possessed ion channel activity. The resultant compounds retained excellent potency and exhibited diminished ion channel activity.

Bioorganic & Medicinal Chemistry Letters published new progress about Anti-inflammatory agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application of C19H34O2.

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

Smyth, Elizabeth; Cozens, Kelly; Griffiths, Daniel; Clark, Kathryn L; Ewings, Sean; Petty, Russell; Underwood, Tim; Fitzgerald, Rebecca C; Tanner, James; Giger, Olivier; Anand, Shubha; Griffiths, Gareth published the artcile< ELEVATE - evaluating Temozolomide and Nivolumab in patients with advanced unresectable previously treated oesophagogastric adenocarcinoma with MGMT methylation: study protocol for a single arm phase II trial.>, Related Products of 112-63-0, the main research area is Immunotherapy; MGMT methylated; Oesophagogastric adenocarcinoma; Phase II.

BACKGROUND: For patients with oesophagogastric adenocarcinoma, surgery is the only curative option and despite the use of multimodality therapy, which combines it with chemotherapy and/or radiotherapy, more than 50% of patients will relapse and die. Many UK patients present with advanced disease which is already inoperable or metastatic at diagnosis. For these patients, standard care chemotherapy only offers them survival of less than a year. Nivolumab, a checkpoint blockade inhibitor, has been found to work in some advanced cancers. It is proposed, for those where immunotherapy hasn’t worked, that these immunologically evasive tumours need to be sensitized to immunotherapy drugs to allow them to act. METHODS: ELEVATE is a single arm phase II trial testing the overall response to nivolumab following temozolomide treatment in patients with advanced unresectable previously treated adenocarcinoma which is O6-methylguanine-DNA-methyltransferase (MGMT) methylated. 18 patients are being recruited from UK secondary care sites. To be eligible, participants must have been treated with at least 3 months of platinum and fluoropyrimidine chemotherapy. Participants will receive 50 mg/m2 temozolomide continuously for 3 months. If their disease progresses during the 3 months, they will stop temozolomide and start nivolumab at a dose of 240mg every 2 weeks. If there is no progression after 3 months the participant will continue taking temozolomide in combination with nivolumab. All treatment will stop once the participant progresses on nivolumab. The primary endpoint is the best overall response to nivolumab, using both Response Evaluation Criteria in Solid Tumours version 1.1 and immunotherapy modified Response Evaluation Criteria in Solid Tumours. Secondary endpoints include progression-free survival, overall survival, and quality of life. DISCUSSION: ELEVATE will provide evidence for whether giving nivolumab after temozolomide in patients with previously treated advanced oesophagogastric adenocarcinoma is safe and biologically effective prior to future randomised trials. TRIAL REGISTRATIONS: EudraCT Number: 2020-004771-41 (issued 01 October 2020); ISCRTN11398887 (registered 14 July 2021).

BMC cancer published new progress about 112-63-0. 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

Lin, Zhixian; Sun, Zhe; Xu, Chengping; Zhang, Aiqin; Xiang, Jun; Fan, Haojun published the artcile< A self-matting waterborne polyurethane coating with admirable abrasion-resistance>, Application of C19H34O2, the main research area is waterborne polyurethane coating abrasion resistance.

Due to the paradox between abrasion-resistance and extinction, the development of a self-matting waterborne polyurethane (SMWPU) coating accompanied by excellent abrasion-resistance is still a challenge. Herein, a kind of hydroxyalkyl-terminated polysiloxane modified SMWPU was prepared and employed for matting leather/synthetic leather finishing. Simultaneously, the influences of hydrophilic chain extender and polysiloxane loadings on the matting effect and abrasion resistance of the coating were investigated in detail. The results indicated that the gloss of the coating was closely related to the hydrophilic chain extender content, and a stable emulsion and optimal matting effect could be achieved when a 1.6 weight% (based on solid content) hydrophilic chain extender was employed. With the introduction of polysiloxane, the silicon element content on the coating surface increased from 0% to 9.26%, just as expected, and an enhanced abrasion resistance of the coating was obtained. Specifically, the coating weight loss ratio was reduced from 2.36 weight% to 0.41 weight%, and obvious surface damage did not occur after 500 abrasions. Although the surface roughness and matting effect of the coating decreased slightly due to the introduction of silicone, the gloss of the modified coating was less than 1.5° (60° incidence angle), still exhibiting an excellent matting effect. Another interesting result was the elevation of anti-hot-pressing, compared with that of the unmodified one, and the gloss of the modified coating showed no changes under a 10 MPa, 150°C hot-pressing condition.

RSC Advances published new progress about Abrasion resistance. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application of C19H34O2.

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

Balakrishnan, Remya; Nallaperumal, Agasthiyalingom Meenakshi; Manu, Saraswathy Kesava Pillai; Varghese, Lity Alen; Sekkar, Venkataraman published the artcile< DSC assisted kinetic analysis on the urethane network formation between castor oil based ester polyol and poly(methylene di phenyl isocyanate) (pMDI)>, Electric Literature of 112-63-0, the main research area is castor oil polyol pMDI urethane network formation kinetics.

Kinetics of the reaction between castor oil based ester polyol (CEP) and poly(methylene di Ph isocyanate) (pMDI) was studied adopting differential scanning calorimetry (DSC). DSC scans were recorded at various heating rates, viz.: 5, 10, 15 and 20 K.min-1. Hydroxyl and isocyanato compounds were taken at stoichiometric ratio [r=[NCO/OH]=1] Both single heating rate methods (Coats-Redfern, Chatterjee-Conrad) and multiple heating rate based iso-conversional methods (Ozawa, Freidman and Kissinger) were adopted to calculate the kinetic parameters. DSC thermograms consist of two exothermic peaks at temperatures 343 and 393 K, for all heating rates. Kinetic parameters were calculated using input parameters deduced from DSC thermogram. The reaction was assumed to be second order and the corresponding second order equations were applied for evaluating the kinetic parameters.

International Journal of Polymer Analysis and Characterization published new progress about Activation energy. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Electric Literature of 112-63-0.

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

Song, Jianling; Zou, Xiaoyan; Liu, Pandao; Cardoso, Juan Andres; Schultze-Kraft, Rainer; Liu, Guodao; Luo, Lijuan; Chen, Zhijian published the artcile< Differential expressions and enzymatic properties of malate dehydrogenases in response to nutrient and metal stresses in Stylosanthes guianensis>, Reference of 112-63-0, the main research area is Stylosanthes malate dehydrogenase nutrient metal stress; Enzymatic properties; Gene expression; Malate; Malate dehydrogenase; Metal stress; Nutrient deficiency; Stylosanthes guianensis.

Malate dehydrogenase (MDH, EC 1.1.1.37) is a key enzyme that catalyzes a reversible NAD-dependent dehydrogenase reaction from oxaloacetate (OAA) to malate. Although MDH has been documented to participate in cellular metabolism and redox homeostasis in plants, the roles of MDH members in the tropical legume Stylosanthes guianensis (stylo) remain less definitive. In this study, except SgMDH1 that had been previously characterized, six novel MDH genes were isolated from stylo and were then designated as SgMDH2 to SgMDH7. All of the SgMDH proteins possessed the common features of NAD binding, dimerization interface and substrate binding sites. Expression anal. showed that three SgMDHs exhibited preferential expressions in leaves, and one SgMDH was mainly expressed in roots. Furthermore, SgMDHs were regulated by nutrient deficiencies in stylo roots, especially for phosphorus (-P) and potassium (-K) deficiencies. Differential responses of SgMDHs to trace metal stress and heavy metal toxicity were observed in stylo roots, suggesting the involvement of SgMDHs in the response of stylo to metal stresses. The six novel SgMDHs were subsequently expressed and purified from Escherichia coli to analyze their biochem. properties. Although SgMDHs exhibited variations in subcellular localizations, each SgMDH protein displayed a high level of catalytic efficiency towards OAA and NADH but a low level of catalytic efficiency towards malate and NAD+. In addition, the activities of recombinant SgMDH proteins were pH-dependent and temperature-sensitive, and exhibited differential regulations by various metal ions. These results together suggest the potential roles of SgMDHs in stylo coping with nutrient and metal stresses. The sequence data of the six novel SgMDHs were deposited in GenBank under accession numbers OK188912, OK188913, OK188914, OK188915, OK188916 and OK188917 for SgMDH2 to SgMDH7, resp.

Plant Physiology and Biochemistry (Issy-les-Moulineaux, France) published new progress about Chlorophylls Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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

Qiu, Di; Zhang, Yan; Wang, Jianbo published the artcile< Direct synthesis of arylboronic pinacol esters from arylamines>, Safety of (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is pinacol arylboronate aryloxaborolane preparation metal free arylamine borylation.

A metal-free synthetic method based on Sandmeyer-type transformation for preparation of arylboronic pinacol esters from easily available aromatic amines as starting materials was described. This novel transformation affords borylation products in good yields under mild reaction conditions. This strategy can be easily carried out in gram-scale, demonstrating the practical usefulness of the method. Moreover, the Sandmeyer-type transformation can be followed by Suzuki-Miyaura cross-coupling reaction without purification of the arylboronate products.

Organic Chemistry Frontiers published new progress about Aromatic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Safety of (9Z,12Z)-Methyl octadeca-9,12-dienoate.

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

Piesche, L.; Hilse, H.; Oehlke, J.; Schroetter, E.; Oehme, P. published the artcile< Substituted picolinic acids as DBH [dopamine β-hydroxylase] inhibitors. Inhibition of dopamine β-hydroxylase and antihypertensive effect>, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is picolinate derivative antihypertensive dopamine hydroxylase; fusarate derivative antihypertensive dopamine hydroxylase; copper complexing picolinate derivative antihypertensive.

Twenty-seven substituted picolinic acids and fusaric acids (I and II, resp.; R = various small groups, as well as halogen) were characterized as weak-to-moderately strong acids which form stable Cu(II) complexes in solution and in the solid state. The concentrations required for 50% inhibition of purified bovine adrenal dopamine β-hydroxylase  [9013-38-1] were 10-6-10-5M; I were stronger inhibitors than II. The inhibition was noncompetitive with respect to tyramine but was transitional between competitive and noncompetitive with respect to ascorbic acid. The mechanism of enzyme inhibition could not be explained solely by a complexing of the enzyme Cu. Most I and II had antihypertensive activity in spontaneously hypertensive rats, but some further increased the blood pressure. No correlation was observed between antihypertensive activity and dopamine β-hydroxylase inhibition.

Pharmazie published new progress about Antihypertensives. 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

Kisszekelyi, Peter; Alammar, Abdulaziz; Kupai, Jozsef; Huszthy, Peter; Barabas, Julia; Holtzl, Tibor; Szente, Lajos; Bawn, Carlo; Adams, Ralph; Szekely, Gyorgy published the artcile< Asymmetric synthesis with cinchona-decorated cyclodextrin in a continuous-flow membrane reactor>, Category: esters-buliding-blocks, the main research area is cinchona cyclodextrin organocatalyst synthesis asym Michael diketone nitrostyrene; synthesis separation integrated flow reactor cinchona cyclodextrin Michael organocatalyst.

This work presents a cyclodextrin-enhanced organocatalytic method from mol. to process design. Cinchona-thiourea and -squaramide catalysts were covalently anchored to inherently large, stable and well-defined permethyl-β-cyclodextrins. The asym. catalysis was successfully demonstrated on the Michael reaction of 1,3-diketones and trans-β-nitrostyrene. Both emerging green and conventional solvents were screened for the asym. addition (up to 99% ee), and the Kamlet-Taft solvent parameters were correlated to the enantioselectivity. Quantum chem. modeling revealed that the catalyst anchoring resulted in favorable structural changes, and stronger intermol. interactions between the catalyst and the reagents. Continuous organocatalysis was performed in coiled tube flow reactor coupled with a membrane separation unit, which allowed complete recovery of the catalyst and 50% solvent (2-MeTHF) recycling. The 100% conversion, 98% purity, 99% ee, 100% in-line catalyst recovery, and 80 g L-1 h-1 productivity makes it an attractive catalytic platform.

Journal of Catalysis published new progress about Addition reaction, stereoselective (catalysts). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Category: esters-buliding-blocks.

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

Xia, Liang; Zhang, Yan; Zhang, Jingbo; Lin, Songwen; Zhang, Kehui; Tian, Hua; Dong, Yi; Xu, Heng published the artcile< Identification of novel thiazolo[5,4-b]pyridine derivatives as potent phosphoinositide 3-kinase inhibitors>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is thiazolopyridine preparation antitumor SAR mol docking phosphoinositide kinase inhibitor; docking analysis; heterocycle; inhibitory potency; phosphoinositide 3-kinase; thiazolo[5,4-b]pyridine.

A series of novel 2-pyridyl, 4-morpholinyl substituted thiazolo[5,4-b]pyridine analogs I [X=CH, N; R1= H, methoxy; R2 = Me, 2,4-difluorophenyl, 5-chloro-2-thienyl, etc.] was designed and synthesized. These thiazolo[5,4-b]pyridines were efficiently prepared in seven steps from com. available substances in moderate to good yields. All of these N-heterocyclic compounds were characterized by NMR and high-resolution mass spectrometry anal. and tested for phosphoinositide 3-kinase (PI3K) enzymic assay. The results indicated that these N-heterocyclic compounds showed potent PI3K inhibitory activity, and the IC50 of a representative compound I [X=N; R1= methoxy; R2= 2,4-difluorophenyl] would reach to 3.6 nm. The structure-activity relationships (SAR) study showed that sulfonamide functionality was important for PI3Kα inhibitory activity, and 2-chloro-4-fluorophenyl sulfonamide I [X=N; R1= methoxy; R2 = 2-chloro-4-fluoro-phenyl] or 5-chlorothiophene-2-sulfonamide I [X=N; R1= methoxy; R2= 5-chloro-2-thienyl] showed potent inhibitory activity with a nanomolar IC50 value. The pyridyl attached to thiazolo[5,4-b]pyridine was another key structural unit for PI3Kα inhibitory potency, and replacement by Ph leaded to a significant decrease in activity. Enzymic Inhibition results showed that compound I [X=N; R1= methoxy; R2= 2,4-difluorophenyl] inhibited PI3Kα, PI3Kγ, or PI3Kδ with a nanomolar IC50 value, but its inhibitory activity on PI3Kβ was approx. 10-fold reduced. Further docking anal. revealed that the N-heterocyclic core of compound I [X=N; R1= methoxy; R2= 2,4-difluorophenyl] was directly involved in the binding to the kinase through the key hydrogen bonds interaction.

Molecules published new progress about Antitumor agents. 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