Category: esters-buliding-blocks

Chen, Shulun; Guo, Wei; Liu, Xiaohua; Sun, Pu; Wang, Yi; Ding, Chunyong; Meng, Linghua; Zhang, Ao published the artcile< Design, synthesis and antitumor study of a series of N-Cyclic sulfamoylaminoethyl substituted 1,2,5-oxadiazol-3-amines as new indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors>, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is cyclic sulfamoylaminoethyloxadiazolamine preparation antitumor indoleamine dioxygenase inhibitor human; Immunotherapy; Indoleamine 2,3-dioxygenase; Life span; Oxadiazole; PD-1.

Indoleamine 2,3-dioxygenase 1 (IDO1) plays a key role in tryptophan catabolism which is an important mechanism in immune tolerance. The small mol. epacadostat is the most advanced IDO1 inhibitor, but its phase III trials as a single agent or in combinations with PD-1 antibody failed to show appreciable objective responses. To gain more insight on the antitumor efficacy of IDO1 inhibitors, a series of analogs of epacadostat by incorporating a cyclic aminosulfonamide moiety as the sidechain capping functionality has been designed. N-(3-bromo-4-fluorophenyl)-4-((2-(1,1-dioxido-1,2,5-thiadiazolidin-2-yl)ethyl)amino)-N’-hydroxy-1,2,5-oxadiazole-3-carboximidamide was found to display significant potency against recombinant hIDO1 and hIDO1 expressed HEK293 cancer cells and this compound has improved physico-chem. properties, acceptable PK parameters as well as optimal cardiac safety. Similar to epacadostat, the above compound is ineffective as single agent in the CT-26 syngeneic xenograft model, however, the combination of this compound with PD-1 antibody showed both elevated tumor growth inhibition and prolonged median life span.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 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

Xu, Weici; Li, Yuanzhen; Liu, Rui; Yang, Shuang; Liu, Jian; Fang, Xinqiang published the artcile< Kinetic resolution of 2,2-disubstituted-1,3-diketones via carbene catalysis>, Application In Synthesis of 112-63-0, the main research area is formylbenzyl diketone carbene catalyst enantioselective regioselective kinetic resolution; formylalkyl diketone carbene catalyst enantioselective regioselective kinetic resolution.

The successful organocatalytic kinetic resolution of 1,3-diketones with central quaternary stereocenters through the introduction of internal nucleophiles was reported. Two basic resolution modes were established, allowing access to a broad scope of enantioenriched 1,3-diketones with quaternary stereocenters, together with a large variety of tetralone derivatives with vicinal fully substituted carbon centers, and both of them were not easily available via currently known methods. The inherent principles between the different combinations of ketone groups and the resolution patterns were also disclosed. This work constituted a good complementary choice for the construction of 1,3-diketones with quaternary stereogenic centers and provided insightful information for further studies on diketone substrate-mediated intramol. annulations and kinetic resolutions

Organic Chemistry Frontiers published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 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

Rogers, Jane E.; Lam, Michael; Halperin, Daniel M.; Dagohoy, Cecile G.; Yao, James C.; Dasari, Arvind published the artcile< Fluorouracil, Doxorubicin with Streptozocin and Subsequent Therapies in Pancreatic Neuroendocrine Tumors>, Electric Literature of 112-63-0, the main research area is fluorouracil doxorubicin streptozocin anticancer pancreatic neuroendocrine cancer; Everolimus; Gastroenteropancreatic neuroendocrine tumors; Neuroendocrine tumors; Pancreatic neoplasms; Streptozocin; Temozolomide.

We evaluated outcomes of treatment with 5-fluorouracil (5-FU), doxorubicin, and streptozocin (FAS) in well-differentiated pancreatic neuroendocrine tumors (PanNETs) and its impact on subsequent therapy (everolimus or temozolomide). Advanced PanNET patients treated at our center from 1992 to 2013 were retrospectively reviewed. Patients received bolus 5-FU (400 mg/m2), streptozocin (400 mg/m2) (both IV, days 1-5), and doxorubicin (40 mg/m2 IV, day 1) every 28 days. Overall response rate (ORR) was assessed using RECIST version 1.1. Of 243 eligible patients, 220 were evaluable for ORR, progression-free survival (PFS), and toxicity. Most (≥90%) had metastatic, nonfunctional PanNETs; 14% had prior therapy. ORR to FAS was 41% (95% confidence interval [CI]: 36-48%). Median follow-up was 61 mo. Median PFS was 20 (95% CI: 15-23) months; median overall survival (OS) was 63 (95% CI: 60-71) months. Cox regression analyses suggested improvement with first-line vs. subsequent lines of FAS therapy. Main adverse events ≥ grade 3 were neutropenia (10%) and nausea/vomiting (5.5%). Dose reductions were required in 32% of patients. Post-FAS everolimus (n = 108; 68% second line) had a median PFS of 10 (95% CI: 8-14) months. Post-FAS temozolomide (n = 60; 53% ≥ fourth line) had an ORR of 13% and median PFS of 5.2 (95% CI: 4-12) months. In this largest reported cohort of PanNETs treated with chemotherapy, FAS demonstrated activity without significant safety concerns. FAS did not appear to affect subsequent PFS with everolimus; this sequence is being evaluated prospectively. Responses were noted with subsequent temozolomide-based regimens although PFS was possibly limited by line of therapy.

Neuroendocrinology published new progress about Antitumor agents. 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

Karve, Aniruddha S.; Desai, Janki M.; Dave, Nimita; Wise-Draper, Trisha M.; Gudelsky, Gary A.; Phoenix, Timothy N.; DasGupta, Biplab; Sengupta, Soma; Plas, David R.; Desai, Pankaj B. published the artcile< Potentiation of temozolomide activity against glioblastoma cells by aromatase inhibitor letrozole>, COA of Formula: C19H34O2, the main research area is Aromatase inhibitors; Drug-resistance; Glioblastoma; Letrozole; Synergism; Temozolomide.

Abstract: Purpose: The DNA alkylating agent temozolomide (TMZ), is the first-line therapeutic for the treatment of glioblastoma (GBM). However, its use is confounded by the occurrence of drug resistance and debilitating adverse effects. Previously, we observed that letrozole (LTZ), an aromatase inhibitor, has potent activity against GBM in pre-clin. models. Here, we evaluated the effect of LTZ on TMZ activity against patient-derived GBM cells. Methods: Employing patient-derived G76 (TMZ-sensitive), BT142 (TMZ-intermediately sensitive) and G43 and G75 (TMZ-resistant) GBM lines we assessed the influence of LTZ and TMZ on cell viability and neurosphere growth. Combination Index (CI) anal. was performed to gain quant. insights of this interaction. We then assessed DNA damaging effects by conducting flow-cytometric anal. of H2A. X formation and induction of apoptotic signaling pathways (caspase3/7 activity). The effects of adding estradiol on LTZ-induced cytotoxicity and DNA damage were also evaluated. Results: Co-treatment with LTZ at a non-cytotoxic concentration (40 nM) reduced TMZ IC50 by 8, 37, 240 and 640 folds in G76, BT-142, G43 and G75 cells, resp. The interaction was deemed to be synergistic based on CI anal. LTZ co-treatment also significantly increased DNA damaging effects of TMZ. Addition of estradiol abrogated these LTZ effects. Conclusions: LTZ increases DNA damage and synergistically enhances TMZ activity in TMZ sensitive and TMZ-resistant GBM lines. These effects are abrogated by the addition of exogenous estradiol underscoring that the observed effects of LTZ may be mediated by estrogen deprivation. Our study provides a strong rationale for investigating the clin. potential of combining LTZ and TMZ for GBM therapy.

Cancer Chemotherapy and Pharmacology published new progress about 112-63-0. 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

Cui, Hai-Lei; Huang, Ji-Rong; Lei, Jie; Wang, Zhao-Feng; Chen, Shi; Wu, Li; Chen, Ying-Chun published the artcile< Direct Asymmetric Allylic Alkylation of Butenolides with Morita-Baylis-Hillman Carbonates>, Safety of (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is Morita Baylis Hillman carbonate butenolide regioselective asym allylic alkylation; cinchona alkaloid catalyst asym allylic alkylation; substituted butenolide stereoselective preparation; bicyclic lactone preparation.

The direct asym. allylic alkylation of β,γ-butenolides with MBH carbonates to access γ,γ-disubstituted butenolides containing adjacent quaternary and tertiary chiral centers, e.g. I, has been presented in excellent stereoselectivities (86-96% ee, dr >95:5) and moderate to good yield (50-83%). Their synthetic utility has been well demonstrated by the facile construction of bicyclic lactones bearing 4-5 stereogenic centers, e.g. II.

Organic Letters published new progress about Allylic alkylation catalysts, stereoselective. 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

Chen, Deyan; Liu, Yang; Zhang, Zetian; Li, Shan; Yang, Kaifeng; Li, Zhengjun published the artcile< Ingeniously incorporating hollow mesoporous silica into waterborne polyurethane film to improve water vapor permeability>, Quality Control of 112-63-0, the main research area is hollow mesoporous silica waterborne polyurethane film.

Incorporating hollow mesoporous silica (HMS) into waterborne polyurethane (WPU) to improve water vapor permeability (WVP) remains a major challenge. Herein, HMS-I and HMS-II with large hollow size and mesoporous structure were prepared with n-hexane as pore-expanding agent, and template was removed by calcination and extraction, resp. Then, HMS/WPU composite emulsion was prepared by dispersing the pre-prepared polyurethane prepolymer terminated by 3-(aminopropyl)triethoxysilane (APTES) into aqueous medium containing HMS particles, with the help of co-condensation between silanol on HMS surface and silanol produced by Si-OEt hydrolysis of APTES. The results showed that the WVP of the composite film was greatly improved, especially HMS-II/WPU was better than HMS-I/WPU. This design strategy provides a prospect for the preparation and extensive application of HMS/WPU functional composites.

Materials Letters published new progress about Calcination. 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

Mapelli, Roberto; Julita, Chiara; Bianchi, Sofia Paola; Gallina, Nicolò; Lucchini, Raffaella; Midulla, Martina; Puci, Flavia; Saddi, Jessica; Trivellato, Sara; Panizza, Denis; De Ponti, Elena; Arcangeli, Stefano published the artcile< Association between treatment-related lymphopenia and survival in glioblastoma patients following postoperative chemoradiotherapy.>, Category: esters-buliding-blocks, the main research area is Glioblastoma; Immunosuppression; Lymphopenia; Radiotherapy; Temozolomide.

PURPOSE: Our study investigated the association between treatment-related lymphopenia and overall survival (OS) in a series of glioblastoma (GBM) patients. We also explored clinical and dosimetric predictors of lymphocytes depletion. METHODS: Between 2015 and 2019, 64 patients were treated at the same institution with postoperative chemoradiotherapy. Peripheral lymphocyte count (PLC) data and dose-volume histogram parameters were collected. Radiotherapy (RT) schedule consisted in standard total dose of 60 Gy in 30 daily fractions, with concomitant and adjuvant temozolomide (TMZ). Posttreatment acute absolute lymphopenia (nadir AAL) was calculated as a PLC lower than 1.0 × 103/mm3. Acute relative lymphopenia (ARL) was expressed by the nadir-PLC/baseline-PLC ratio < 0.5. Nadir-PLC was the lowest PLC registered between the end of RT and the first month of follow-up. Survival rates were estimated with Kaplan-Meier curves. Clinical and dosimetric variables related to AAL/ARL and OS were identified by univariate and multivariate analyses. RESULTS: A total of 57 patients were eligible and included in the analyses. The median PLC was significantly decreased following chemoradiotherapy (2180/mm3 vs 900/mm3). Median OS was 16 months (range 5-55 months), with no significant difference between patients who developed nadir AAL and those who did not (16 months vs 16.5 months; p = 0.304). When considering ARL vs non-ARL, median OS was 14 months vs 26 months (p = 0.013), respectively. In multivariate Cox regression only age, sex, extent of surgery, access to adjuvant chemotherapy and brain D98% were independently associated with OS. CONCLUSION: Although iatrogenic immunosuppression could be associated with inferior clinical outcomes, our data show that treatment-related lymphopenia does not adversely affect GBM survival. Prospective studies are required to confirm these findings. Strahlentherapie und Onkologie : Organ der Deutschen Rontgengesellschaft ... [et al] published new progress about 112-63-0. 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

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

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

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