Tag: M.W=250-300

Schnoeller, Leon Emanuel; Albrecht, Valerie; Brix, Nikko; Nieto, Alexander Edward; Fleischmann, Daniel Felix; Niyazi, Maximilian; Hess, Julia; Belka, Claus; Unger, Kristian; Lauber, Kirsten; Orth, Michael published the artcile< Integrative analysis of therapy resistance and transcriptomic profiling data in glioblastoma cells identifies sensitization vulnerabilities for combined modality radiochemotherapy>, Application In Synthesis of 112-63-0, the main research area is human glioblastoma cell therapy resistance transcriptomics radiochemotherapy; ATM; ATR; Chemosensitization; Clonogenic survival; Correlation analysis; DNA damage response; Glioblastoma; LIG4; Radiosensitization; Radiotherapy; Temozolomide; Therapy resistance.

Inherent resistance to radio/chemotherapy is one of the major reasons for early recurrence, treatment failure, and dismal prognosis of glioblastoma. Thus, the identification of resistance driving regulators as prognostic and/or predictive markers as well as potential vulnerabilities for combined modality treatment approaches is of pivotal importance. We performed an integrative anal. of treatment resistance and DNA damage response regulator expression in a panel of human glioblastoma cell lines. mRNA expression levels of 38 DNA damage response regulators were analyzed by qRT-PCR. Inherent resistance to radiotherapy (single-shot and fractionated mode) and/or temozolomide treatment was assessed by clonogenic survival assays. Resistance scores were extracted by dimensionality reduction and subjected to correlation analyses with the mRNA expression data. Top-hit candidates with pos. correlation coefficients were validated by pharmacol. inhibition in clonogenic survival assays and DNA repair analyses via residual γH2AX/53BP1-foci staining. Inherent resistance to single-shot and similarly also to fractionated radiotherapy showed strong pos. correlations with mRNA expression levels of known vulnerabilities of GBM, including PARP1, NBN, and BLM, as well as ATR and LIG4-two so far underestimated targets. Inhibition of ATR by AZD-6738 resulted in robust and dose-dependent radiosensitization of glioblastoma cells, whereas LIG4 inhibition by L189 had no noticeable impact. Resistance against temozolomide showed strong pos. correlation with mRNA expression levels of MGMT as to be expected. Interestingly, it also correlated with mRNA expression levels of ATM, suggesting a potential role of ATM in the context of temozolomide resistance in glioblastoma cells. ATM inhibition exhibited slight sensitization effects towards temozolomide treatment in MGMT low expressing glioblastoma cells, thus encouraging further characterization. Here, we describe a systematic approach integrating clonogenic survival data with mRNA expression data of DNA damage response regulators in human glioblastoma cell lines to identify markers of inherent therapy resistance and potential vulnerabilities for targeted sensitization. Our results provide proof-of-concept for the feasibility of this approach, including its limitations. We consider this strategy to be adaptable to other cancer entities as well as other mol. data qualities, and its upscaling potential in terms of model systems and observational data levels deserves further investigation.

Radiation Oncology published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (ATR). 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

Wu, Xiaoting; Qi, Xiaoyi; Wang, Jing; Zhang, Yunying; Xiao, Yanwei; Tu, Caixia; Wang, Aoxue published the artcile< Paeoniflorin attenuates the allergic contact dermatitis response via inhibiting the IFN-γ production and the NF-κB/IκBα signaling pathway in T lymphocytes>, Computed Properties of 112-63-0, the main research area is paeoniflorin attenuate allergic dermatitis inhibiting IFNG NFkB IkBa signaling; Allergic contact dermatitis; Mice; NF-κB signaling pathway; Paeoniflorin; T lymphocytes.

Paeoniflorin (PF) has been demonstrated to have an anti-allergic and anti-inflammatory effect in the treatment of allergic contact dermatitis (ACD). However, its clin. application is hampered by the lacking of comprehensive mech. explanation. This research aimed to study the effect of PF on the proliferation, apoptosis and cytokines secretion as well as the expression of nuclear factor-kappa B (NF-κB) and mitogen-activated protein kinase (MAPK) signaling pathways of T lymphocytes activation in vitro and in vivo. We found that PF depressed human T lymphocytes activation via inhibition of interferon-gamma (IFN-γ) production and NF-κB/IκBα and p38 MAPK signaling pathway in vitro, also PF could attenuate such ACD responses by inhibiting the production of IFN-γ and NF-κB/IκBα pathway in T lymphocytes of ACD mouse model, suggesting that PF might be useful for the treatment of T cell-mediated allergic inflammatory disorders such as ACD. This would make PF a promising T cell-targeted drug candidate for further study because of its immunosuppressive and anti-inflammatory effects.

International Immunopharmacology published new progress about Allergic contact dermatitis. 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

Kvasnica, M.; Oklestkova, J.; Bazgier, V.; Rarova, L.; Korinkova, P.; Mikulik, J.; Budesinsky, M.; Beres, T.; Berka, K.; Lu, Q.; Russinova, E.; Strnad, M. published the artcile< Design, synthesis and biological activities of new brassinosteroid analogues with a phenyl group in the side chain>, COA of Formula: C19H34O2, the main research area is brassinolide analog preparation plant hormone antitumor agent cytotoxicity; etiolated pea seedlings plant hormone ethylene production differences.

We have prepared and studied a series of new brassinosteroid derivatives with a p-substituted Ph group in the side chain. To obtain the best comparison between mol. docking and biol. activities both types of brassinosteroids were synthesized; 6-ketones, 10 examples, and B-lactones, 8 examples. The Ph group was introduced into the steroid skeleton by Horner-Wadsworth-Emmons. The docking studies were carried out using AutoDock Vina 1.05. Plant biol. activities were established using different brassinosteroid bioassays in comparison with natural brassinosteroids. Differences in the production of the plant hormone ethylene were also observed in etiolated pea seedlings after treatment with new brassinosteroids. The most active compounds were lactone I and 6-oxo derivatives II [R2 = H, F], their biol. activities were comparable or even better than naturally occurring brassinolide. Finally the cytotoxicity of the new derivatives was studied using human normal and cancer cell lines.

Organic & Biomolecular Chemistry published new progress about Antiproliferative agents (weak to moderate). 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

Whitehead, Daniel C.; Fhaner, Matthew; Borhan, Babak published the artcile< A peptide bromoiodinane approach for asymmetric bromolactonization>, SDS of cas: 112-63-0, the main research area is bromomethylphenyltetrahydrofuranone enantioselective preparation; phenylpentenoic acid asym bromolactonization iodoarylpeptide catalyst; iodoarylpeptide solid phase preparation bromolactonization.

A series of 37 peptides containing an iodo-aryl amide active site were generated by means of both solid phase and conventional synthesis. These peptides were screened for asym. induction in the bromolactonization of 4-phenyl-4-pentenoic acid based on the generation of chiral bromoiodinane bromenium sources. The study culminated in the discovery of a tri-peptide iodo-aryl amide that effected the desired bromolactonization in quant. conversion with 24% ee. The experiments disclosed herein provided valuable insight that ultimately facilitated the development of more synthetically useful enantioselective halocyclization methodol.

Tetrahedron Letters published new progress about Enantioselective synthesis. 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

Rozsar, Daniel; Formica, Michele; Yamazaki, Ken; Hamlin, Trevor A.; Dixon, Darren J. published the artcile< Bifunctional Iminophosphorane Catalyzed Enantioselective Sulfa-Michael Addition to Unactivated α,β-Unsaturated Amides>, Application In Synthesis of 112-63-0, the main research area is bifunctional iminophosphorane catalyst preparation potential energy surface; unsaturated amide thiol iminophosphorane catalyst enantioselective Michael addition; thioamide preparation.

The first metal-free catalytic intermol. enantioselective Michael addition to unactivated α,β-unsaturated amides was described. Consistently high enantiomeric excesses and yields were obtained over a wide range of alkyl thiol pronucleophiles and electrophiles under mild reaction conditions, enabled by a novel squaramide-based bifunctional iminophosphorane (BIMP) catalyst. Low catalyst loadings (2.0 mol %) were achieved on a decagram scale, demonstrating the scalability of the reaction. Computational anal. revealed the origin of the high enantiofacial selectivity via anal. of relevant transition structures and provided substantial support for specific noncovalent activation of the carbonyl group of the α,β-unsaturated amide by the catalyst.

Journal of the American Chemical Society published new progress about Enantioselective synthesis. 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

Cabaj, John E.; Kairys, David; Benson, Thomas R. published the artcile< Development of a Commercial Process to Produce Oxandrolone>, Related Products of 112-63-0, the main research area is Oxandrolone preparation.

A manufacturing scale process for the preparation of the anabolic steroid Oxandrolone was developed. Key elements included the following: the bromination of methylandrostanolone with perbromide to give the 2-bromoketone in ca. 80% yield with minimal dehydration, subsequent elimination of the bromide with Li2CO3/LiBr to give the 2-enone in ca. 70% yield with minimal formation of methyltestosterone, and an ozonolysis procedure to give the penultimate intermediate in ca. 90% yield. The overall yield from methylandrostanolone to Oxandrolone using the described process was 45% as compared to the original Searle yield of 8%.

Organic Process Research & Development published new progress about Bromination. 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

Scheuerman, R. A.; Tumelty, D. published the artcile< The reduction of aromatic nitro groups on solid supports using sodium hydrosulfite (Na2S2O4)>, Category: esters-buliding-blocks, the main research area is reduction aromatic nitro group hydrosulfite solid support; polyethyleneglycol polystyrene resin reduction nitroarom hydrosulfite; tin dichloride reduction nitroarom solid support.

An improved method for reducing aromatic nitro compounds on solid-phase supports using sodium hydrosulfite is presented. Conditions have been optimized to enable the use of this reagent for reductions on both polyethyleneglycol-polystyrene resins and traditional polystyrene resins.

Tetrahedron Letters published new progress about Aromatic amines Role: SPN (Synthetic Preparation), PREP (Preparation). 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

Matsuda, Shoichi; Yamaguchi, Shoji; Yasukawa, Eiki; Asahina, Hitoshi; Kakuta, Hirofumi; Otani, Haruhiko; Kimura, Shin; Kameda, Takashi; Takayanagi, Yoshiki; Tajika, Akihiko; Kubo, Yoshimi; Uosaki, Kohei published the artcile< Effect of Electrolyte Filling Technology on the Performance of Porous Carbon Electrode-Based Lithium-Oxygen Batteries>, Computed Properties of 112-63-0, the main research area is lithium oxygen batteries electrolyte carbon electrode.

Although the theor. energy densities of lithium-oxygen batteries (LOBs) far exceed those of lithium-ion batteries, the practical values of the LOBs are usually much lower because of the use of large electrolyte excesses. Thus, to realize LOBs with a high practical energy d., the electrolyte amount should be minimized without compromising their performance. To address this challenge, we herein investigate the influence of several electrolyte filling techniques on the performance of LOBs, revealing that the battery discharge/charge profiles are strongly influenced by the uniformity of electrolyte distribution in the porous carbon electrode. The obtained results show the importance of electrolyte filling technol. for realization of practical high-energy-d. LOBs and facilitate their further development.

ACS Applied Energy Materials published new progress about Battery electrodes. 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

Dong, Jianyang; Yue, Fuyang; Liu, Jianhua; Song, Hongjian; Liu, Yuxiu; Wang, Qingmin published the artcile< Visible-light-mediated three-component Minisci reaction for heteroarylethyl alcohols synthesis>, HPLC of Formula: 112-63-0, the main research area is heteroarylethyl alc green diastereoselective preparation; heteroaryl alkene three component Minisci visible light iridium catalyst.

Herein, a mild, modular, practical Minisci reaction for catalytic synthesis of heteroarylethyl alcs. such as ArCH(R1)CHR2OH [Ar = quinol-2-yl, isoquinolin-1-yl, 2-benzothiazolyl, etc.; R1R2 = CH2(CH2)2CH2, CH2CH2CH2; R1 = On-Bu, Me; R2 = H, Me] via sequential addition of H2O and N-heteroarenes across olefinic double bonds was reported. This scalable protocol was used for direct hydroxy-heteroarylation of olefins with a wide range of N-heteroarenes and could be expected to permit rapid conversion of abundant feedstock materials into medically relevant mols.

Green Chemistry published new progress about Alcohols Role: SPN (Synthetic Preparation), PREP (Preparation) (heteroarylethyl). 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

Zhang, Wei; Guo, Xiaoli; Ren, Jing; Chen, Yujiao; Wang, Jingyu; Gao, Ai published the artcile< GCN5-mediated PKM2 acetylation participates in benzene-induced hematotoxicity through regulating glycolysis and inflammation via p-Stat3/IL17A axis>, Reference of 112-63-0, the main research area is GCN5 PKM2 acetylation benzene hematotoxicity glycolysis inflammation Stat3 IL17A; Acetylation; Benzene; Glycolysis; Hematotoxicity; Inflammation; PKM2.

Benzene is a common environmental carcinogen that induces leukemia. Studies suggest that metabolic disorder has a relationship with the toxicity of benzene. Pyruvate kinase M2 (PKM2) is a key rate-limiting enzyme in glycolysis. However, the upstream and downstream regulatory mechanisms of PKM2 in benzene-induced hematotoxicity and the therapeutic effects of targeting PKM2 in vivo are unclear. This study aims to provide insights into the new mechanism of benzene-induced hematotoxicity and reveal the therapeutic significance of targeting PKM2. Herein, we demonstrated that PKM2-dependent glycolysis contributes to benzene-induced hematotoxicity by regulating inflammation reaction. Mechanistically, acetylated proteomics revealed that 1,4-benzoquinone (1,4-BQ) induced acetylation of PKM2 at position K66, and this modification contributed to the increase of PKM2 expression and can be inhibited by inhibition of acetyltransferase GCN5. Meanwhile, the elevated PKM2 was shown to prompt the activation of nuclear phosphorylated Stat3 (p-Stat3) and IL17A. Clin., pharmacol. inhibition of PKM2 alleviated the blood toxicity induced by benzene, which was mainly characterized by an increase in routine blood parameters and improvement of hematopoietic imbalance. Besides, elevated PKM2 is a promising biomarker in people occupationally exposed to benzene. Overall, we identified PKM2/p-Stat3/IL-17A axis participates in the hematotoxicity of benzene, and targeting PKM2 has certain therapeutic implications in hematol. diseases.

Environmental Pollution (Oxford, United Kingdom) published new progress about Acetylation. 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