Month: October 2022

Lustig, Samuel D.; Kodali, Sravan K.; Longo, Sharon L.; Kundu, Somanath; Viapiano, Mariano S. published the artcile< Ko143 reverses MDR in glioblastoma via deactivating P-glycoprotein, sensitizing a resistant phenotype to TMZ treatment>, Quality Control of 112-63-0, the main research area is reverses MDR glioblastoma deactivating P glycoprotein phenotype temozolomide treatment; BCRP; Ko143; P-glycoprotein; combinatorial treatment; drug resistance; temozolomide.

Over-expression of both P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP) has been associated with multidrug-resistance in glioblastoma (GBM). Though previously studied broad-spectrum inhibitors of drug efflux pumps have failed to progress in clin. studies due to in vivo toxicity, research into clin. viable targeted inhibitors is needed. This study evaluated the effects of Ko143, a non-toxic analog of fumitremorgin C, on temozolomide (TMZ) efficacy in resistant glioblastoma stem cells. We used ATP-Glo assay to determine cell viabilities and flow cytometry to perform cell cycle anal. Comparative gene expression was analyzed through RT-qPCR. TMZ IC50 decreased 41.07% (p<0.01) in the resistant phenotype when delivered in combination with Ko143. Addnl., the TMZ-resistant phenotype (GBM146) displayed 44-fold greater P-gp expression than the TMZ-sensitive phenotype (GBM9) (p<0.01), yet a 0.6-fold lower BCRP expression. Ko143 potentiates TMZ efficacy and likely inhibits P-glycoprotein more potently than previously indicated. Further development of non-toxic, targeted inhibitors of drug efflux pumps for use in combinatorial chemotherapy may improve glioblastoma patient prognosis. Anticancer Research published new progress about Antitumor agents. 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

Mingoia, Francesco published the artcile< Reactivity of 5-(3-azidophenyl)-1-(1H-pyrrol-3-yl)pyrroles in TFMSA. A route for new ring systems as DNA-interactive agents>, Formula: C7H10N2O2, the main research area is azidophenyl pyrrolylpyrrole preparation cyclization; dipyrroloisoquinoline preparation DNA interactive agent.

Acid catalyzed decomposition of 5-(3-azidophenyl)-1-(1H-pyrrol-3-yl)pyrroles did not afford the expected dipyrrolo[2,1-a:3,4-c]isoquinoline derivatives, but the planar dipyrrolo[2,1-a:3,2-c]isoquinoline derivatives and related non planar derivatives H-dipyrrolo[2,1-a:3,2-c]isoquinoline derivatives In strong acid media (trifluoromethanesulfonic acid) the α-(1-pyrrol-3-yl) position even if blocked, was more prone to undergo cyclization with respect to the free β one. Despite the steric hindrance, these compounds were obtained in moderate to good overall yields, depending on the nature and position of the substituents on the 1-(1H-pyrrolyl) moiety.

Tetrahedron published new progress about DNA Role: MSC (Miscellaneous). 252932-48-2 belongs to class esters-buliding-blocks, and the molecular formula is C7H10N2O2, Formula: C7H10N2O2.

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

Qaid, Mohammed M.; Mansour, Lamjed; Al-Garadi, Maged A.; Alqhtani, Abdulmohsen H.; Al-abdullatif, Abdulaziz A.; Qasem, Mahmood A.; Murshed, Mutee A. published the artcile< Evaluation of the anticoccidial effect of traditional medicinal plants, Cinnamomum verum bark and Rumex nervosus leaves in experimentally infected broiler chickens with Eimeria tenella>, Electric Literature of 112-63-0, the main research area is CNB Rumex nervosus leaf broiler Eimeria tenella anticoccidial plant.

Rumex nervosus leaves (RNL) and Cinnamomum verum bark (CNB), phytogenic herbs, have received much attention in recent years for their antimicrobial properties; however, there is limited knowledge about their potential anticoccidial functions. The prophylactic effects of RNL and CNB were compared with salinomycin, a standard synthetic anticoccidial agent, in broilers exptl. infected with Eimeria tenella (E. tenella). One-day-old broiler chicks (n = 225) were randomly divided into nine groups. Birds were either fed a basal diet containing 1, 3, or 5 g RNL or 2, 4, or 6 g CNB/kg feed, or treated with salinomycin within the basal diet, or the infected (IUT) or non-infected (UUT) groups were fed a basal diet only. Birds infected (n = 25 bird/group) with 40,000 sporulated E. tenella oocysts/bird at d 21 except UUT. Bodweight gain (BWG) and feed conversion ratio (FCR) were significantly (p < .05) lower in IUT compared to UUT. On day 7 post-infection (DPI), birds treated with RNL, CNB, or salinomycin had fewer lesions in the caeca and a lower oocyst value, and a higher oocyst reduction rate in the faeces than birds in the IUT. Although RNL was not able to reduce weight loss caused by coccidiosis, CNB at 6 g improved FCR and production efficiency index (PEI) at 7 DPI compared to the infected groups. In conclusion, RNL at 5 g and CNB at 6 g have moderate anti-coccidial activity and could be used to treat poultry coccidiosis in the field. However, more research is needed to identify active ingredients that make it effective compared to com. available drugs. HIGHLIGHTSPhytogenic feed additives prevented weight loss and caecum pathol. in broiler chickens at risk of coccidiosis. Rumex nervosus leaves and Cinnamomum verum bark had similar effects to the coccidiostat salinomycin at high doses. Traditional medicinal plants are potential alternatives to pharmaceutical coccidiostats to promote the health and growth of broiler chickens. Italian Journal of Animal Science published new progress about Antimicrobial 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

Richter, Hans G. F.; Adams, D. R.; Benardeau, A.; Bickerdike, M. J.; Bentley, J. M.; Blench, T. J.; Cliffe, I. A.; Dourish, C.; Hebeisen, P.; Kennett, G. A.; Knight, A. R.; Malcolm, C. S.; Mattei, P.; Misra, A.; Mizrahi, J.; Monck, N. J. T.; Plancher, J.-M.; Roever, S.; Roffey, J. R. A.; Taylor, S.; Vickers, S. P. published the artcile< Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT2C receptor agonists>, SDS of cas: 112-63-0, the main research area is pyridopyrrolopyrazine preparation 5HT agonist.

Further lead optimization efforts on previously described 1,2,3,4,10,10a-hexahydro-1H-pyrazino[1,2-a]indoles led to the new class of 5,5a,6,7,8,9-hexahydro-pyrido[3′,2′:4,5]pyrrolo[1,2-a]pyrazines culminating in the discovery of (5aR,9R)-2-[(cyclopropylmethoxy)methyl]-5,5a,6,7,8,9-hexahydro-9-methyl-pyrido[3′,2′:4,5]pyrrolo[1,2-a]pyrazine as a potent, full 5-HT2C receptor agonist with an outstanding selectivity profile and excellent hERG and phospholipidosis properties.

Bioorganic & Medicinal Chemistry Letters published new progress about 5-HT2C receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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

Klement, Rainer J.; Popp, Ilinca; Kaul, David; Ehret, Felix; Grosu, Anca L.; Polat, Buelent; Sweeney, Reinhart A.; Lewitzki, Victor published the artcile< Accelerated hyper-versus normofractionated radiochemotherapy with temozolomide in patients with glioblastoma: a multicenter retrospective analysis>, Reference of 112-63-0, the main research area is glioblastoma temozolomide HFRT NFRT survival MGMT hypermethylation IDH mutation; Accelerated hyperfractionation; Altered fractionation; Glioblastoma; Radiotherapy; Temozolomide.

The standard treatment of glioblastoma patients consists of surgery followed by normofractionated radiotherapy (NFRT) with concomitant and adjuvant temozolomide chemotherapy. Whether accelerated hyperfractionated radiotherapy (HFRT) yields comparable results to NFRT in combination with temozolomide has only sparsely been investigated. The objective of this study was to compare NFRT with HFRT in a multicenter anal. A total of 484 glioblastoma patients from four centers were retrospectively pooled and analyzed. Three-hundred-ten and 174 patients had been treated with NFRT (30 x 1.8 Gy or 30 x 2 Gy) and HFRT (37 x 1.6 Gy or 30 x 1.8 Gy twice/day), resp. The primary outcome of interest was overall survival (OS) which was correlated with patient-, tumor- and treatment-related variables via univariable and multivariable Cox frailty models. For multivariable modeling, missing covariates were imputed using multiple imputation by chained equations, and a sensitivity anal. was performed on the complete-cases-only dataset. After a median follow-up of 15.7 mo (range 0.8-88.6 mo), median OS was 16.9 mo (15.0-18.7 mo) in the NFRT group and 14.9 mo (13.2-17.3 mo) in the HFRT group (p = 0.26). In multivariable frailty regression, better performance status, gross-total vs. not gross-total resection, MGMT hypermethylation, IDH mutation, smaller planning target volume and salvage therapy were significantly associated with longer OS (all p < 0.01). Treatment differences (HFRT vs. NFRT) had no significant effect on OS in either univariable or multivariable anal. Since HFRT with temozolomide was not associated with worse OS, we assume HFRT to be a potential option for patients wishing to shorten their treatment time. Journal of Neuro-Oncology published new progress about Aging, animal. 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

Chalyk, Bohdan A.; Isakov, Andrei A.; Butko, Maryna V.; Hrebeniuk, Kateryna V.; Savych, Olena V.; Kucher, Olexandr V.; Gavrilenko, Konstantin S.; Druzhenko, Tetiana V.; Yarmolchuk, Vladimir S.; Zozulya, Sergey; Mykhailiuk, Pavel K. published the artcile< Synthesis of 6-Azaspiro[4.3]alkanes: Innovative Scaffolds for Drug Discovery>, COA of Formula: C19H34O2, the main research area is azaspiroalkane preparation; alkene benzylazomethine ylide cycloaddition.

New scaffolds for drug discovery, 6-azaspiro[4.3]alkanes, I (R = H, F; A = O, S, SO2, etc.; EWG = COOEt, CN, NO2, etc.) have been synthesized in two steps from four-membered-ring ketones: cyclobutanone, thienone, N-Boc-azetidinone (Boc = tert-butoxycarbonyl), etc. The key transformation was the reaction between electron-deficient exocyclic alkenes and an in-situ generated N-benzylazomethine ylide.

European Journal of Organic Chemistry published new progress about [3+2] Cycloaddition reaction. 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

Zhang, Yan; Lv, Jie; Zhang, Suqing; Yang, Hanxi; Shen, Jingshan; Du, Changsheng; Jiang, Xiangrui; Aisa, Haji A. published the artcile< Synthesis and biological evaluation of artemisinin derivatives as potential MS agents>, Product Details of C19H34O2, the main research area is artemisinin derivative anti multiple sclerosis agent; Artemisinin derivatives; EAE; IFN-γ/IL-17A; Multiple sclerosis; Th1/Th17.

In this paper, a series of artemisinin derivatives were synthesized and evaluated. Studies have shown that IFN-γ produced by Th1 CD4+ T cells and IL-17A secreted by Th17 CD4+ T cells played critical roles in the treatment of multiple sclerosis. We used different concentrations of artemisinin derivatives to inhibit Th1 / Th17 differentiation in naive CD4+ T cells and to characterize IFN-γ / IL-17A in in vitro experiments The preliminary screening results showed that ester compound 5 (I) exhibited obvious inhibitory activities on Th1 and Th17 (IFN-γ decreased from 41% to 3% and IL-17A decreased from 24% to 8% at the concentration of 10 nM to 10μM), and carbamate compounds also had obvious inhibitory activities against Th17 at high concentration Moreover, we investigated the effect of compound 5 on myelin oligodendrocyte glycoprotein (MOG)-induced mice exptl. autoimmune encephalomyelitis (EAE) model in vivo. 100 mg/kg compound 5 effectively reduced the disease severity of EAE compared with the vehicle group. This research revealed that compound 5 could be a promising avenue as potential MS inhibitor.

Bioorganic & Medicinal Chemistry Letters published new progress about Anti-multiple sclerosis agents. 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

Choi, Woonghee; Kang, Yongku; Kim, In-Jung; Seong, Byeong-Gi; Yu, Woong-Ryeol; Kim, Dong Wook published the artcile< Stable Cycling of a 4 V Class Lithium Polymer Battery Enabled by In Situ Cross-Linked Ethylene Oxide/Propylene Oxide Copolymer Electrolytes with Controlled Molecular Structures>, Formula: C19H34O2, the main research area is stable cycling lithium polymer battery ethylene propylene oxide electrolyte; 4 V class lithium polymer batteries; electrochemical stability; ethylene oxide/propylene oxide copolymer; in situ cross-linking; solid polymer electrolytes.

Com. lithium-ion batteries are vulnerable to fire accidents, mainly due to volatile and flammable liquid electrolytes. Although solid polymer electrolytes (SPEs) are considered promising alternatives with antiflammability and processability for roll-to-roll mass production, several requirements have not yet been fulfilled for a viable lithium polymer battery. Such requirements include ionic conductivity, electrochem. stability, and interfacial resistance. In this work, the ionic conductivity of the SPEs is optimized by controlling the mol. weight and structural morphol. of the plasticizers as well as introducing propylene oxide (PO) groups. Electrochem. stability is also enhanced using ethylene oxide (EO)/PO copolymer electrolytes, making the SPEs compatible with high-Ni LiNixCoyMn1-x-yO2 cathodes. The in situ crosslinking method, in which a liquid precursor first wets the electrode and is then solidified by a subsequent thermal treatment, enables the SPEs to soak into the 60μm thick electrode with a high loading d. of more than 8 mg cm-2. Thus, interfacial resistance between the SPE and the electrode is minimized. By using the in situ cross-linked EO/PO copolymer electrolytes, we successfully demonstrate a 4 V class lithium polymer battery, which performs stable cycling with a marginal capacity fading even over 100 cycles.

ACS Applied Materials & Interfaces published new progress about Battery capacity. 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

Das, Krishna Kumar; Jha, Sunil Kumar; Pattanaik, Gurudutta; Sharma, Yangya Prasad Nath; Behera, Santosh Kumar published the artcile< In silico analysis and network pharmacology of the impact of genes associated with multidrug-resistant tuberculosis (MDR-TB)>, Reference of 112-63-0, the main research area is gene network multidrug resistance tuberculosis.

Drug-resistant tuberculosis (DR-TB) continues to be a public health crisis worldwide during 2018. It estimates approx. 5,58,000 cases (range, 4,83,000-s6,39,000) developed TB resistant to rifampicin (RR-TB). The most effective first line drug, and of these, 82% had multidrug-resistant TB (MDR-TB). Three countries accounted for almost half of the world’s cases of MDR/RR-TB: India (24%), China (13%) and the Russian Federation (10%). Ample of studies were performed in India, based on the previously informed mutations, in addition to which several novel mutations were also observed in the genes such as rpoB (rifampicin), katG, the ribosomal binding site of inhA (isoniazid), gyrA and gyrB (ofloxacin), rpsL and rrs (streptomycin). The current investigation was carried out to explore the gene-gene interaction which are supposed to be the master regulators in MDR-TB. A total of 12 genes were mined from 618 publications in MalaCard which are responsible for MDR-TB. STRING network database reported the genes namely IL10, SLC11A1, TNF, DEFA3, DEFA1 at the core region of the network which are supposed to play a key role in TB. These genes may be also responsible for differentially expressed in MDR-TB disease. The Drug association anal. of Web Gestalt has reported 15 drugs interacted with 12 genes. In the current investigation we would like to suggest for further in vivo and in silico anal. of the reported genes for therapeutics of MDR-TB.

World Journal of Pharmaceutical Research published new progress about Animal gene Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study) (ACVR2A). 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

Vila, Carlos; Dharmaraj, Nisshanth Raj; Faubel, Antonio; Blay, Gonzalo; Cardona, M. Luz; Munoz, M. Carmen; Pedro, Jose R. published the artcile< Regio-, Diastereo-, and Enantioselective Organocatalytic Addition of 4-Substituted Pyrazolones to Isatin-Derived Nitroalkenes>, Category: esters-buliding-blocks, the main research area is pyrazolone nitroalkene organocatalyst regioselective enantioselective diastereoselective nucleophilic vinylic substitution; chiral alkenylpyrazolone stereoselective preparation; hydroquinine diphenyl pyrimidinediyl diether catalyst.

Hydroquinine 2,5-diphenyl-4,6-pyrimidinediyl diether [(DHQ)2Pyr] catalyzed the regio-, diastereo-, and enantioselective addition of 4-substituted pyrazolones to isatin-derived nitroalkenes, providing a variety of chiral alkenylpyrazolone adducts, e.g., I, containing a tetrasubstituted stereocenter bearing an oxindole moiety with excellent yields, regioselectivity, and diastereoselectivity, as well as a moderate enantioselectivity (up to 98 % yield, > 20:1 E/Z ratio dr and 78 % ee). The reaction harnesses a nitroalkene as an alkenylating agent through a Nucleophilic Vinylic Substitution (SNV) reaction.

European Journal of Organic Chemistry published new progress about Alkenes, nitro Role: RCT (Reactant), RACT (Reactant or Reagent) (isatin-derived). 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