Month: November 2022

Huang, Wei-Sheng; Liu, Shuangying; Zou, Dong; Thomas, Mathew; Wang, Yihan; Zhou, Tianjun; Romero, Jan; Kohlmann, Anna; Li, Feng; Qi, Jiwei; Cai, Lisi; Dwight, Timothy A.; Xu, Yongjin; Xu, Rongsong; Dodd, Rory; Toms, Angela; Parillon, Lois; Lu, Xiaohui; Anjum, Rana; Zhang, Sen; Wang, Frank; Keats, Jeffrey; Wardwell, Scott D.; Ning, Yaoyu; Xu, Qihong; Moran, Lauren E.; Mohemmad, Qurish K.; Jang, Hyun Gyung; Clackson, Tim; Narasimhan, Narayana I.; Rivera, Victor M.; Zhu, Xiaotian; Dalgarno, David; Shakespeare, William C. published the artcile< Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is brigatinib antitumor neoplasm anaplastic lymphoma kinase inhibitor.

In the treatment of echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase pos. (ALK+) non-small-cell lung cancer (NSCLC), secondary mutations within the ALK kinase domain have emerged as a major resistance mechanism to both first- and second-generation ALK inhibitors. This report describes the design and synthesis of a series of 2,4-diarylaminopyrimidine-based potent and selective ALK inhibitors culminating in identification of the investigational clin. candidate brigatinib. A unique structural feature of brigatinib is a phosphine oxide, an overlooked but novel hydrogen-bond acceptor that drives potency and selectivity in addition to favorable ADME properties. Brigatinib displayed low nanomolar IC50s against native ALK and all tested clin. relevant ALK mutants in both enzyme-based biochem. and cell-based viability assays and demonstrated efficacy in multiple ALK+ xenografts in mice, including Karpas-299 (anaplastic large-cell lymphomas [ALCL]) and H3122 (NSCLC). Brigatinib represents the most clin. advanced phosphine oxide-containing drug candidate to date and is currently being evaluated in a global phase 2 registration trial.

Journal of Medicinal Chemistry published new progress about Antitumor agent resistance. 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

Cao, Xu-Liang; Hewitt, C. Nicholas published the artcile< Gas chromatographic determination of volatile alkenes with on-column bromination and electron-capture detection>, Computed Properties of 112-63-0, the main research area is gas chromatog volatile alkene oncolumn bromination.

A method is described for the gas chromatog.-electron-capture detection determination of alkenes via on-column bromination reactions. Pyridinium bromide perbromide (PBPB) was used as the Br2 source, and a cholesterol-glass beads mixture, treated with MeOH, was used to remove excess Br2. The optimum ratio of cholesterol to glass beads is 1:10, at which 93% of the Br released from PBPB can be removed, without removal of the derivatized analytes. The conversion efficiency of alkene to the brominated derivative is extremely low (<2%) for ethene, whereas for propene and 1-butene it is 41 and 79%, resp. For C3-C5 alkenes, this method is 200-300 times more sensitive than anal. of the underivatized analytes by using conventional flame ionization detection. Journal of Chromatography A published new progress about Alkenes Role: ANT (Analyte), ANST (Analytical Study). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Computed Properties of 112-63-0.

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

Zhao, Mingming; Yang, Bin; Li, Liusheng; Si, Yuan; Chang, Meiying; Ma, Sijia; Li, Ronghai; Wang, Yuejun; Zhang, Yu published the artcile< Efficacy of Modified Huangqi Chifeng decoction in alleviating renal fibrosis in rats with IgA nephropathy by inhibiting the TGF-β1/Smad3 signaling pathway through exosome regulation>, COA of Formula: C19H34O2, the main research area is IgA nephropathy exosome Huangqi Chifeng decoction TGFbeta1 Smad3 signaling; Exosomes; IgA nephropathy; Modified Huangqi Chifeng decoction; Renal fibrosis; TGF-β1/Smad3 signaling pathway.

IgA nephropathy is the most common form of primary glomerulonephritis and is a major cause of renal failure worldwide. Modified Huangqi Chifeng decoction (MHCD), a traditional Chinese herbal preparation, has clin. efficacy in reducing the 24-h urine protein levels in patients with IgA nephropathy. However, the mol. mechanism of MHCD needs further study. This study aimed to investigate the mechanisms by which MHCD treatment alleviates renal fibrosis. An IgA nephropathy rat model was established using bovine serum albumin, carbon tetrachloride, and lipopolysaccharide. The rats were divided into control, model, telmisartan, low-dose MHCD, medium-dose MHCD, and high-dose MHCD groups. Treatments were administered to these groups for 8 wk. Subsequently, the 24-h urine protein, serum creatinine, blood urea nitrogen, and blood albumin levels were measured. Pathol. changes and degree of fibrosis in renal tissues were observed, and levels of the transforming growth factor-β1 (TGF-β1)/Smad3 signaling pathway components in renal tissues and TGF-β1 in urinary exosomes were measured. Telmisartan and MHCD reduced 24-h urine protein levels, alleviated renal pathol. injury, and decreased the renal expression of fibronectin, laminin, and collagen IV in rats with IgA nephropathy. Urinary exosomes were extracted and identified for further investigation of their role in renal fibrosis. MHCD reduced TGF-β1 expression in urinary exosomes and reduced TGF-β1 and p-Smad3 levels in renal tissues. MHCD alleviated renal fibrosis in rats with IgA nephropathy by inhibiting the TGF-β1/Smad3 signaling pathway through the downregulation of TGF-β1 expression in exosomes.

Journal of Ethnopharmacology published new progress about Autoimmune glomerulonephritis. 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

Braddock, D. Christopher; Cansell, Gemma; Hermitage, Stephen A.; White, Andrew J. P. published the artcile< Bromoiodinanes with an I(III)-Br bond: preparation, X-ray crystallography and reactivity as electrophilic brominating agents>, Computed Properties of 112-63-0, the main research area is bromoiodinane crystallog reactivity electrophilic brominating agent.

Bromoiodinanes – conveniently and directly prepared from iodobenzenecarbinols and N-bromosuccinimide, and characterized for the first time crystallog. – act as electrophilic bromine donors.

Chemical Communications (Cambridge, United Kingdom) published new progress about Bond length (I(III)-Br). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Computed Properties of 112-63-0.

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

Min, Xu; Dingchao, Xiang; Xun, Zhu; Cunzu, Wang published the artcile< Preliminary Study on Relationship Between Temozolomide Chemotherapy-Resistant Cells and Stem Cells in Gliomas.>, SDS of cas: 112-63-0, the main research area is .

AIM: To study the relationship between temozolomide (TMZ) chemotherapy-resistant cells and stem cells in gliomas. MATERIAL AND METHODS: The U251 glioma cell line was exposed to TMZ to generate TMZ-resistant colonies (U251/TMZ cell line) using the pulse drug method. The TMZ sensitivity of U251/TMZ and parental cells was examined using an MTT assay. The cell growth curve was drawn to show the growth of the two kinds of cells. Glioma stem cells (GSCs) were cultured and differentiated in vitro. Immunofluorescence assays were used to identify the expression of CD133, Nestin, and ABCG2 in U251/TM and U251 cells. Western blot analysis was used to analyse protein expression levels. RESULTS: The U251/TMZ cell line was successfully cultured in vitro. The IC50 value of the U251/TMZ cell line is 8.1 times that of the parental U251 cell line (t=-63.28, p=0.00). The doubling time of U251/TMZ cells was long compared with the parental cells. GSC tumour spheres were successfully cultured in vitro, and they differentiated in medium containing serum. The expression of CD133, Nestin, and ABCG2 in U251/TMZ cells was significantly higher than that in the parental U251 cells (t=43.35, p=0.00; t=12.31, p=0.00; t=11.49, p=0.00). Immunofluorescence staining of CD133, Nestin, and ABCG2 was significantly higher in U251/TMZ than in the parental U251 cells (t=43.35, p=0.00; t=12.31, p=0.00; t=11.49, p=0.00). Moreover, Western blot results showed that CD133, Nestin, and ABCG2 expression was significantly higher in U251/TMZ cells than that in the parental U251 cells (t=17.76, p=0.00; t=18.78, p=0.00; t=6.19, p=0.00). CONCLUSION: The U251/TMZ cell line has the biological characteristics of GSCs. The relationship between GSCs and chemotherapy-resistant cells has been preliminary proven to be partially overlapping, which can provide a new perspective when using appropriate cell subpopulations as targets for glioma.

Turkish neurosurgery published new progress about 112-63-0. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, SDS of cas: 112-63-0.

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

Ognyanov, Vassil I.; Balan, Chenera; Bannon, Anthony W.; Bo, Yunxin; Dominguez, Celia; Fotsch, Christopher; Gore, Vijay K.; Klionsky, Lana; Ma, Vu V.; Qian, Yi-Xin; Tamir, Rami; Wang, Xianghong; Xi, Ning; Xu, Shimin; Zhu, Dawn; Gavva, Narender R.; Treanor, James J. S.; Norman, Mark H. published the artcile< Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles>, HPLC of Formula: 112-63-0, the main research area is benzimidazole piperazinyl preparation transient receptor potential vanilloid antagonist antihyperalgesic.

The vanilloid receptor-1 (VR1 or TRPV1) is a membrane-bound, nonselective cation channel that is predominantly expressed by peripheral neurons sensing painful stimuli. TRPV1 antagonists produce antihyperalgesic effects in animal models of inflammatory and neuropathic pain. The synthesis and the structure-activity relationships of a series of 2-(4-pyridin-2-ylpiperazin-1-yl)-1H-benzo[d]imidazoles I [R1 = H, Me3SiCH2CH2OCH2, PhCH2; R2 = F, Cl, Br, F3C, Me, CN, Me3C, MeO2C, etc.; R3 = H, 4-(2-thiazolyl), 4-(4-pyridyl), 5-(4-F3CC6H4), etc.; R4 = H, Me; R5 = H, H2N, MeCHOH, H2C:CH, etc.; R6 = H, Cl, F3C, etc.] and analogs as novel TRPV1 antagonists have been described. I [R1 = H; R2 = F3C; R3 = 4-(3,4,5-F3C6H2); R4 = (R)-Me; R5 = HOCH2CHOH; R6 = Cl; (II)] was among the most potent analogs in this series. This compound was orally bioavailable in rats and was efficacious in blocking capsaicin-induced flinch in rats in a dose-dependent manner. II also reversed thermal hyperalgesia in a model of inflammatory pain, which was induced by complete Freund’s adjuvant (CFA).

Journal of Medicinal Chemistry published new progress about Analgesics. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, HPLC of Formula: 112-63-0.

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

Yin, Qi; Wen, Xiaolu; Chen, Yiwei; Gong, Xiangnan; Hu, Lin published the artcile< Phase-Transfer Catalyzed Asymmetric [4 + 1] Annulations for the Synthesis of Chiral 2,2-Disubstituted Tetrahydrothiophenes>, Application In Synthesis of 94-02-0, the main research area is succinimidothiopentenoate tert butyl keto ester cinchona catalyst; tert butyl carboxyl tetrahydrothiophene preparation enantioselective diastereoselective.

An efficient catalytic asym. [4 + 1] reaction, which features the use of simple β-keto esters as one-carbon nucleophiles and 5-succinimidothio-pent-2-enoates as four-atom bielectrophiles, was developed in the presence of a bifunctional chiral phase-transfer catalyst. The new annulation provided a distinct protocol to access the functionalized 2-acyl-2-carboxyl tetrahydrothiophenes bearing consecutive quaternary and tertiary carbon stereocenters in high diastereoselectivities and enantioselectivities. Moreover, the prepared products could be readily transformed into the chiral 2-alkyl-2-carboxyl tetrahydrothiophenes via two steps of debenzoylation and alkylation reactions.

Organic Letters published new progress about [4+1] Cycloaddition reaction. 94-02-0 belongs to class esters-buliding-blocks, and the molecular formula is C11H12O3, Application In Synthesis of 94-02-0.

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

Allingham, Matthew T.; Howard-Jones, Andrew; Murphy, Patrick J.; Thomas, Dafydd A.; Caulkett, Peter W. R. published the artcile< Synthesis and applications of C2-symmetric guanidine bases>, Synthetic Route of 617-55-0, the main research area is sym guanidine base preparation phase transfer catalyst enantioselective transformation.

The preparation of the tetracyclic C2-sym. guanidinium salts I·BF4- (R = Me, CH2OSiMe2CMe3, CH2OSiPh2CMe3) is reported together with their application to enantioselective transformations, such their effectiveness as phase-transfer catalysts.

Tetrahedron Letters published new progress about Aldol condensation catalysts, stereoselective. 617-55-0 belongs to class esters-buliding-blocks, and the molecular formula is C6H10O5, Synthetic Route of 617-55-0.

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

Maddox, Sean M.; Dawson, Gregory A.; Rochester, Nicholas C.; Ayonon, Arianna B.; Moore, Curtis E.; Rheingold, Arnold L.; Gustafson, Jeffrey L. published the artcile< Enantioselective Synthesis of Biaryl Atropisomers via the Addition of Thiophenols into Aryl-Naphthoquinones>, Product Details of C19H34O2, the main research area is enantioselective synthesis biaryl atropisomer thiophenol addition arylnaphthoquinone; aryl-naphthoquinone; atroposelective; biaryl atropisomers; cinchona alkaloid; thiophenol.

We report a cinchona alkaloid catalyzed addition of thiophenol into rapidly interconverting aryl-naphthoquinones, resulting in stable biaryl atropisomers upon reductive methylation. An array of thiophenols and naphthoquinone substrates were evaluated, and we observed selectivities up to 98.5:1.5 e.r. Control of the quinone redox properties allowed us to study the stereochem. stabilities of each oxidation state of the substrates. The resulting enantioenriched products can also be moved on via an SNAr-like reaction sequence to arrive at stable derivatives with excellent enantioretention.

ACS Catalysis published new progress about Atropisomers. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Product Details of C19H34O2.

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

Jiang, Xinglong; Prasad, Kapa; Repic, Oljan published the artcile< Synthesis of fused bicyclo[3.2.2]nonenones>, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is benzamide methyl lithiation substitution cyclohexanecarboxylate; pyridine amide methyl lithiation substitution cyclohexanecarboxylate; isoquinolinone preparation; naphthyridinone annelated bicyclononenone preparation; fused heterocycle preparation.

The 2H-isoquinolin-1-one- and 7H-[1,7]naphthyridin-8-one-annelated title compounds were prepared from 2-methylbenzoic acid t-butylamide or 3-methyl-2-pyridinecarboxylic acid t-butylamide via lithiation, reaction of intermediate carbanions with monomethyl 1,4-cyclohexanedicarboxylate, and dehydration/cyclization of resulting 2- or 3-(4-carboxycyclohexanylcarbonyl)methyl derivatives with polyphosphoric acid.

Organic Preparations and Procedures International published new progress about Fused heterocyclic compounds Role: SPN (Synthetic Preparation), PREP (Preparation). 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