Tag: M.W=100-150

I found the field of Oncology very interesting. Saw the article Real-life results from the overall population and key subgroups within the Italian cohort of nivolumab expanded access program in non-squamous non-small cell lung cancer published in 2019.0. Quality Control of 1-Phenylurea, Reprint Addresses Grossi, F (corresponding author), Fdn IRCCS Ca Granda Osped Maggiore Policlin, Med Oncol Unit, Milan, Italy.. The CAS is 64-10-8. Through research, I have a further understanding and discovery of 1-Phenylurea

Background: Nivolumab was the first immune checkpoint inhibitor approved for previously treated advanced nonesmall cell lung cancer (NSCLC). Before its introduction in the market, nivolumab was made available to NSCLC patients through an expanded access program (EAP). Here we present the Italian cohort of patients with non-squamous NSCLC enrolled in a worldwide nivolumab EAP, with subgroup analyses involving elderly patients, patients with central nervous system (CNS) metastases and patients receiving nivolumab beyond progression. Methods: Pretreated patients with advanced non-squamous NSCLC received nivolumab at 3 mg/kg every 2 weeks up to 24 months. Efficacy data (investigator-assessed tumour response, progression date and survival) and safety data were collected. Findings: 1588 patients were treated across 153 Italian centres. Overall response rate and disease control rate were 18% and 44%, respectively; median overall survival (OS) was 11.3 months (95% CI: 10.2-12.4). Elderly patients (>= 70 n = 522; >= 75 n = 232) achieved outcomes similar to the global study population; patients with CNS metastases (n = 409) had an OS of 8.6 months (95% CI: 6.4-10.8), and a 1-year OS rate of 43%. Nivolumab was administered beyond progression to 276 patients (26%), 57 of whom achieved subsequent disease control; the median OS of patients receiving nivolumab beyond progression was 16.2 months (95% CI: 14.0-18.4), while 1-year OS rate was 62%. Interpretation: To date, this is the largest clinical experience with nivolumab in a real-world setting. Our data support its use in clinical practice for pretreated non-squamous NSCLC, including patients with older age or CNS metastases. (C) 2019 Elsevier Ltd. All rights reserved.

Quality Control of 1-Phenylurea. Welcome to talk about 64-10-8, If you have any questions, you can contact Grossi, F; Genova, C; Crino, L; Delmonte, A; Turci, D; Signorelli, D; Passaro, A; Parra, HS; Catino, A; Landi, L; Gelsomino, F; Tiseo, M; Puppo, G; Roila, F; Ricciardi, S; Tonini, G; Cognetti, F; Toschi, L; Tassinari, D; Scoppola, A; Giannarelli, D; Cortesi, E or send Email.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Authors Xie, ZB; Li, HX; Liu, LS; Lan, J; Hu, ZY; Le, ZG in SCIENCE PRESS published article about ONE-POT SYNTHESIS; ENZYME; 2,3-DIHYDROQUINAZOLIN-4(1H)-ONES; EFFICIENT; NANOCATALYST; PROMISCUITY; ACYLASE; MILD in [Xie, Zongbo; Li, Hongxia; Liu, Liansheng; Lan, Jin; Hu, Zhiyu; Le, Zhanggao] East China Univ Technol, Dept Appl Chem, Nanchang 330013, Jiangxi, Peoples R China in 2019, Cited 41. Recommanded Product: 2-Aminobenzamide. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6

Alkaline protease-catalyzed synthesis of quinazolinone derivatives was developed between beta-keotester and o-aminobenzamide. Because ethanol is one kind of eco-friendly solvents, this method can reduce the impact of solvents on the environment. Alkaline protease as a biocatalyst has many advantages, e.g. high catalytic activity, environmentally friendly, wide variety of sources and simple operation. In addition, a variety of quinazolinone derivatives was obtained with good to excellent yields just using 2000 U alkaline protease as catalyst.

Recommanded Product: 2-Aminobenzamide. Welcome to talk about 88-68-6, If you have any questions, you can contact Xie, ZB; Li, HX; Liu, LS; Lan, J; Hu, ZY; Le, ZG or send Email.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Recently I am researching about MICROFIBRILLATED CELLULOSE; POLYMER NANOCOMPOSITES; ELASTIC-MODULUS; MECHANICAL-PROPERTIES; CRYSTALLINE REGIONS; SURFACE; GREEN; DISSOLUTION; BIOCOMPOSITES; NANOCELLULOSE, Saw an article supported by the National Agriculture and Food Research Organization (NARO) Bio-oriented Technology Research Advancement Institution; JSPS KAKENHIMinistry of Education, Culture, Sports, Science and Technology, Japan (MEXT)Japan Society for the Promotion of ScienceGrants-in-Aid for Scientific Research (KAKENHI) [17H06238]; DIC Corporation; Daio Paper Corporation. COA of Formula: C7H8N2O. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Sakakibara, K; Moriki, Y; Tsujn, Y. The CAS is 64-10-8. Through research, I have a further understanding and discovery of 1-Phenylurea

Production of nanocomposites from macro-scale materials in situ in a melting compounder is highly desirable yet challenging. In this study, we develop a highly efficient approach for the preparation of cellulose nanofiber (CNF)-reinforced high-density polyethylene (HDPE) composite materials from as-received wood pulp fibers, in which nanofibrillation-assisting plasticizers (urea and urea derivatives) and a diblock copolymer dispersant are used. The most effective plasticizer is urea, which plays a crucial role in producing CNF with less fragmentation during the kneading step, owing to the plasticization/nanofibrillation and the reaction with hydroxyl groups of cellulose fibers into a carbamate. The diblock copolymer as a dispersant enables the stabilization of the appropriate dispersion of the produced CNF in nonpolar HDPE. The resulting composites exhibit significantly improved mechanical properties, including a 6.9-fold increase in the Youngs modulus with 10 wt % loading of wood pulp fibers over that of neat HDPE.

COA of Formula: C7H8N2O. Welcome to talk about 64-10-8, If you have any questions, you can contact Sakakibara, K; Moriki, Y; Tsujn, Y or send Email.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Computed Properties of C7H8N2O. In 2019 EUR J MED CHEM published article about RESISTANCE PROTEIN BCRP/ABCG2; MULTIDRUG-RESISTANCE; SELECTIVE INHIBITORS; DRUG-RESISTANCE; HIGHLY POTENT; CANCER; TRANSPORTER; BCRP; EXPRESSION; CELLS in [Krapf, Michael K.; Gallus, Jennifer; Spindler, Anna; Wiese, Michael] Univ Bonn, Inst Pharmaceut, Immenburg 4, D-53121 Bonn, Germany in 2019, Cited 51. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6.

Multidrug resistance (MDR) is a major obstacle for effective chemotherapeutic treatment of cancer frequently leading to failure of the therapy. MDR is often associated with the overexpression of ABC transport proteins like ABCB1 or ABCG2 which efflux harmful substances out of cells at the cost of ATP hydrolysis. One way to overcome MDR is to apply potent inhibitors of ABC transporters to restore the sensitivity of the cells toward cytostatic agents. This study focusses on the synthesis and evaluation of novel 2,4-disubstituted quinazoline derivatives regarding the structure-activity-relationship (SAR), their ability to reverse MDR and their mode of interaction with ABCG2. Hence, the inhibitory potency and selectivity toward ABCG2 was determined. Moreover, the intrinsic cytotoxicity and the reversal of MDR were investigated. Interaction type studies with the substrate Hoechst 33342 and conformational analyses of ABCG2 with 5D3 monoclonal antibody were performed for a better understanding of the underlying mechanisms. In our study we could further enhance the inhibitory effect against ABCG2 (compound 31, IC50: 55 nM) and identify the structural features that are crucial for inhibitory potency, the impact on transport activity and binding to the protein. (C) 2018 Elsevier Masson SAS. All rights reserved,

Computed Properties of C7H8N2O. About 2-Aminobenzamide, If you have any questions, you can contact Krapf, MK; Gallus, J; Spindler, A; Wiese, M or concate me.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article Chemical proteomics reveals target selectivity of clinical Jak inhibitors in human primary cells WOS:000488481500022 published article about CYCLIN-DEPENDENT KINASE; DRUG TARGET; OFF-TARGET; KINOME; MUTATION; IDENTIFICATION; TOFACITINIB; RUXOLITINIB; DISCOVERY; PLACEBO in [Eberl, H. Christian; Werner, Thilo; Reinhard, Friedrich B.; Lehmann, Stephanie; Thomson, Douglas; Rau, Christina; Muelbaier, Marcel; Drewes, Gerard; Bantscheff, Marcus] Cellzome GmbH, Meyerhofstr 1, D-69117 Heidelberg, Germany; [Chen, Peiling; Zhang, Cunyu] GlaxoSmithKline, 709 Swedeland Rd 1539, King Of Prussia, PA 19406 USA; [Drewry, David] GlaxoSmithKline, 5 Moore Dr, Res Triangle Pk, NC 27709 USA; [Drewry, David] Univ North Carolina Chapel Hill, UNC Eshelman Sch Pharm, Struct Genom Consortium, 120 Mason Farm Rd, Chapel Hill, NC 27599 USA in 2019, Cited 60. Quality Control of 2-Aminobenzamide. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6

Kinobeads are a set of promiscuous kinase inhibitors immobilized on sepharose beads for the comprehensive enrichment of endogenously expressed protein kinases from cell lines and tissues. These beads enable chemoproteomics profiling of kinase inhibitors of interest in dose-dependent competition studies in combination with quantitative mass spectrometry. We present improved bead matrices that capture more than 350 protein kinases and 15 lipid kinases from human cell lysates, respectively. A multiplexing strategy is suggested that enables determination of apparent dissociation constants in a single mass spectrometry experiment. Miniaturization of the procedure enabled determining the target selectivity of the clinical BCR-ABL inhibitor dasatinib in peripheral blood mononuclear cell (PBMC) lysates from individual donors. Profiling of a set of Jak kinase inhibitors revealed kinase off-targets from nearly all kinase families underpinning the need to profile kinase inhibitors against the kinome. Potently bound off-targets of clinical inhibitors suggest polypharmacology, e.g. through MRCK alpha and beta, which bind to decernotinib with nanomolar affinity.

Welcome to talk about 88-68-6, If you have any questions, you can contact Eberl, HC; Werner, T; Reinhard, FB; Lehmann, S; Thomson, D; Chen, PL; Zhang, CY; Rau, C; Muelbaier, M; Drewes, G; Drewry, D; Bantscheff, M or send Email.. Quality Control of 2-Aminobenzamide

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Recently I am researching about MOLECULAR-OXYGEN; EFFICIENT; 2,3-DIHYDROQUINAZOLIN-4(1H)-ONES; OXIDATION; ALKENES; DERIVATIVES; DESIGN; FACILE; CYCLIZATION; OZONOLYSIS, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [11765002, 21966003]; Science and Technology Project of Jiangxi [20192BBH80012]. HPLC of Formula: C7H8N2O. Published in ROYAL SOC CHEMISTRY in CAMBRIDGE ,Authors: Xie, ZB; Lan, J; Yan, LY; Chen, XH; Li, Q; Meng, J; Le, ZG. The CAS is 88-68-6. Through research, I have a further understanding and discovery of 2-Aminobenzamide

This is the first report on a facile tandem route for synthesizing quinazolinones at room temperature from various aminobenzamides and in situ-generated aldehydes. The latter was formed via C=C bond cleavage, and the overall reaction proceeded using molecular oxygen as a clean oxidant in the absence of a photocatalyst. Visible light, which was indispensable for the entire course of the reaction, played multiple roles. It initially cleaved styrene to an aldehyde, then facilitated its cyclization with an o-substituted aniline, and finally promoted the dehydrogenation of the cyclized intermediate. The previous step provided the feedstock for the next step in the reaction, thereby preventing volatilization, oxidation, and polymerization of the aldehyde. Thus, the overall process is simple, environmentally benign, and economically feasible.

HPLC of Formula: C7H8N2O. Welcome to talk about 88-68-6, If you have any questions, you can contact Xie, ZB; Lan, J; Yan, LY; Chen, XH; Li, Q; Meng, J; Le, ZG or send Email.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Quality Control of 2-Aminobenzamide. Authors Huang, TL; Wang, T; Shi, YS; Chen, J; Guo, XY; Lai, RZ; Liu, XX; Wu, ZP; Peng, DX; Wang, LY; Li, H; Hai, L; Wu, Y in AMER CHEMICAL SOC published article about in [Huang, Tianle; Wang, Ting; Shi, Yuesen; Chen, Jian; Guo, Xiaoyu; Lai, Ruizhi; Liu, Xuexin; Wu, Zhouping; Peng, Dongxue; Wang, Longyu; Li, Hao; Hai, Li; Wu, Yong] Sichuan Univ, Sichuan Engn Lab Plant Sourced Drug & Sichuan Res, West China Sch Pharm, Key Lab Drug Targeting & Drug Delivery Syst,Educ, Chengdu 610041, Peoples R China; [Huang, Tianle; Wang, Ting; Shi, Yuesen; Chen, Jian; Guo, Xiaoyu; Lai, Ruizhi; Liu, Xuexin; Wu, Zhouping; Peng, Dongxue; Wang, Longyu; Li, Hao; Hai, Li; Wu, Yong] Sichuan Univ, Sichuan Res Ctr Drug Precis Ind Technol, West China Sch Pharm, Chengdu 610041, Peoples R China in 2021, Cited 30. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6

Inspired by the diversity created by nature, organic chemists have been using a divergent strategy to improve the synthetic efficiency of diverse molecules. Transition-metal-catalyzed C-H functionalization has become one of the most straightforward, powerful, and atom-economical methods to construct complex scaffolds. However, C-H activation initiated divergent transformation to prepare diverse molecules is still limited. To address this challenge, we herein developed Rh(III)-catalyzed C-H olefination/annulation reaction cascades to divergently construct diverse polyheterocycles by tuning manipulations of directing groups (DGs). Up to 9 distinct scaffolds were creatively synthesized under simple conditions with good functional group tolerance, chemo-, and regioselectivity. Such a versatile strategy and its extension may encourage researchers to discover more promising manipulations of DGs for transition-metal-catalyzed C-H bond activation, making diverse available targets and materials that would have been previously out of range.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article Iridium(III)-Catalyzed Alkynylation of 2-(Hetero)arylquinazolin-4-one Scaffolds via C-H Bond Activation WOS:000460491600052 published article about CROSS-COUPLING REACTION; TERMINAL ALKYNES; ETHYNYL BENZIODOXOLONES; CATALYZED ALKYNYLATION; SONOGASHIRA REACTIONS; ARENES; QUINAZOLINONE; AMIDATION; ACETYLENE; AMINATION in [Rohokale, Rajendra S.; Kalshetti, Rupali G.; Ramana, Chepuri V.] CSIR Natl Chem Lab, Div Organ Chem, Dr Homi Bhabha Rd, Pune 411008, Maharashtra, India; [Kalshetti, Rupali G.; Ramana, Chepuri V.] Acad Sci & Innovat Res, New Delhi 110025, India in 2019, Cited 80. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6. Computed Properties of C7H8N2O

The directed C-H alkynylation of 2-(hetero)arylquinazolin-4-ones has been explored with the ethynylbenziodoxolone reagent TIPS-EBX employing an Ir(III) catalyst. Complementary conditions for either monoalkynylation or dialkynylation have been developed. Also demonstrated is the broad scope of this reaction and the compatibility of various functional groups such as -F, -Cl, -Br, -CF3, -OMe, -NO2, and alkyl, etc.

Computed Properties of C7H8N2O. About 2-Aminobenzamide, If you have any questions, you can contact Rohokale, RS; Kalshetti, RG; Ramana, CV or concate me.

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Application In Synthesis of 2-Aminobenzamide. In 2019 CHINESE CHEM LETT published article about BIOLOGICAL-ACTIVITIES; MANNICH-BASES; DESIGN; ANTIFUNGAL; FLUORINE; PRODUCT; ANALOGS in [Chen, Xiulei; Jia, Haowu; Li, Zhong; Xu, Xiaoyong] East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China; [Li, Zhong; Xu, Xiaoyong] Shanghai Collaborat Innovat Ctr Biomfg Technol, Shanghai 200237, Peoples R China in 2019, Cited 24. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6.

To explore new skeleton with nematicidal activity, a series of novel 1,2,3-benzotriazin-4-one derivatives containing piperazine as linker were synthesized and varied fragments were also introduced to increase structure diversity of the new skeleton. Their inhibitory activities in vivo were evaluated against Meloidogyne incognita. The newly prepared compounds A6, A8, A21, A28 and A38 exhibited more than 50% inhibition at the concentration of 20 mg/L. Especially compound A6 displayed 71.4% inhibition against Meloidogyne incognita at the concentration of 20 mg/L. The nematicidal activities varied significantly depending on the types and positions of the substituents, which provided guidance for further structure modification. (C) 2019 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.

Welcome to talk about 88-68-6, If you have any questions, you can contact Chen, XL; Jia, HW; Li, Z; Xu, XY or send Email.. Application In Synthesis of 2-Aminobenzamide

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Shiota, M; Endo, S; Fujimoto, N; Tsukahara, S; Ushijima, M; Kashiwagi, E; Takeuchi, A; Inokuchi, J; Uchiumi, T; Eto, M in [Shiota, Masaki; Tsukahara, Shigehiro; Ushijima, Miho; Kashiwagi, Eiji; Takeuchi, Ario; Inokuchi, Junichi; Eto, Masatoshi] Kyushu Univ, Grad Sch Med Sci, Dept Urol, Fukuoka, Japan; [Endo, Satoshi] Gifu Pharmaceut Univ, Dept Biopharmaceut Sci, Lab Biochem, Gifu, Japan; [Fujimoto, Naohiro] Univ Occupat & Environm Hlth, Sch Med, Dept Urol, Kitakyushu, Fukuoka, Japan; [Tsukahara, Shigehiro; Uchiumi, Takeshi] Kyushu Univ, Grad Sch Med Sci, Dept Clin Chem & Lab Med, Fukuoka, Japan published Polymorphisms in androgen metabolism genes with serum testosterone levels and prognosis in androgen-deprivation therapy in 2020.0, Cited 36.0. Quality Control of 1-Phenylurea. The Name is 1-Phenylurea. Through research, I have a further understanding and discovery of 64-10-8.

Objective: Androgen metabolism is a key component in therapeutic resistance to androgen deprivation therapy (ADT). This study aimed to reveal the significance of genetic polymorphisms in genes involved in androgen metabolism, including CYP17A1, AKR1C3, and HSD17B, on serum testosterone levels during ADT, as well as the prognosis of men undergoing ADT for metastatic prostate cancer (CaP). Materials and methods: This study included 104 Japanese patients with metastatic CaP, for whom serum testosterone data during ADT were available for 80 patients. The association of CYP17A1 (rs743572), AKR1C3 (rs12529), HSD17B1 (rs605059), HSD17B3 (rs2066479), and HSD17B4 (rs7737181) with serum testosterone levels during ADT and prognosis (progression-free survival and overall survival) was examined. Enzymatic activity in AKR1C3 H5Q was examined using recombinant protein. Results: Homozygous wild-type (GG allele; median [interquartile range], 12.0 ng/ml [8.0-19.0 ng/ml]) AKR1C3 rs12529 was associated with higher serum testosterone levels during ADT compared with variant-type (GC/CC alleles; median [interquartile range], 9.0 ng/ml [6.4-10.8 ng/ml]). Consistently, variant-type (GC/CC alleles) AKR1C3 rs12529 showed significantly lower risk of progression (hazard ratio [95% confidence interval], 0.47 [0.24-0.96], P = 0.039) compared with homozygous wild-type (GG allele) on multivariate analysis. Meanwhile, other genetic variations were associated with neither serum testosterone during ADT nor prognosis. Enzyme activity of wild-type AKR1C3 was comparable to the H5Q mutant. Conclusions: Taken together, this study demonstrated that AKR1C3 polymorphism, which was associated with serum testosterone levels during ADT, may be a prognostic factor of the progression to castration-resistant prostate cancer in Japanese men with metastatic CaP. (C) 2020 Elsevier Inc. All rights reserved.

Welcome to talk about 64-10-8, If you have any questions, you can contact Shiota, M; Endo, S; Fujimoto, N; Tsukahara, S; Ushijima, M; Kashiwagi, E; Takeuchi, A; Inokuchi, J; Uchiumi, T; Eto, M or send Email.. Quality Control of 1-Phenylurea

Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem