Category: 88-68-6

Recently I am researching about HUMAN CYTOCHROME-P450 ENZYMES; IN-VITRO; CANCER-RISK; ESTROGEN METABOLISM; DRUG; HYDROXYLATION; POLYMORPHISM; DERIVATIVES; VALIDATION; INITIATION, Saw an article supported by the UKIERI; HEIF-UK; CYP-Design Ltd.; UGC-UKIERI; UGCUniversity Grants Commission, India [201516-MANF-2015-17-MAH-60712]; DST-FISTDepartment of Science & Technology (India) [SR/FST/CSI-242/2012]. Published in ELSEVIER SCIENCE BV in AMSTERDAM ,Authors: Sonawane, VR; Siddique, MUM; Gatchie, L; Williams, IS; Bharate, SB; Jayaprakash, V; Sinha, BN; Chaudhuri, B. The CAS is 88-68-6. Through research, I have a further understanding and discovery of 2-Aminobenzamide. HPLC of Formula: C7H8N2O

Microsomal cytochrome P450 (CYP) enzymes, isolated from recombinant bacterial/insect/yeast cells, are extensively used for drug metabolism studies. However, they may not always portray how a developmental drug would behave in human cells with intact intracellular transport mechanisms. This study emphasizes the usefulness of human HEK293 kidney cells, grown in ‘suspension’ for expression of CYPs, in finding potent CYP1A1/CYP1B1 inhibitors, as possible anticancer agents. With live cell-based assays, quinazolinones 9i/9b were found to be selective CYP1A1/CYP1B1 inhibitors with IC50 values of 30/21 nM, and > 150-fold selectivity over CYP2/3 enzymes, whereas they were far less active using commercially-available CYP1A1/CYP1B1 microsomal enzymes (IC50, > 10/1.3-1.7 mu M). Compound 9i prevented CYP1A1-mediated benzo [a]pyrene-toxicity in normal fibroblasts whereas 9b completely reversed cisplatin resistance in PC-3/prostate, COR-L23/1ung, MIAPaCa-2/pancreatic and LS174T/colon cancer cells, underlining the human-cell-assays’ potential. Our results indicate that the most potent CYP1A1/CYP1B1 inhibitors would not have been identified if one had relied merely on microsomal enzymes.

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

Name: 2-Aminobenzamide. I found the field of Chemistry; Crystallography very interesting. Saw the article The first example of the stereoselective synthesis and crystal structure of a spirobicycloquinazolinone based on (-)-fenchone and anthranilamide published in 2019, Reprint Addresses Chernyshov, VV (corresponding author), NN Vorozhtsov Novosibirsk Inst Organ Chem SB RAS, 9 Acad Lavrentiev Ave, Novosibirsk 630090, Russia.; Chernyshov, VV (corresponding author), Novosibirsk State Univ, Pirogova St 2, Novosibirsk 630090, Russia.. The CAS is 88-68-6. Through research, I have a further understanding and discovery of 2-Aminobenzamide.

The possibility of a single-stage solvent-free stereoselective synthesis of a spirocyclic compound from the natural bicyclic monoterpenoid (-)-fenchone and anthranilamide has been shown for the first time. The molecular and crystal structure of (1R,2S,4S)-1,3,3-trimethyl-10H-spiro[bicyclo[2.2.1]heptane-2,2′-quinazolin]-4′(3’H)-one, C17H22N2O, was established by X-ray diffraction though the chirality was assumed via the known reactant connectivity and H-1 and C-13 NMR spectroscopy. It has shown that in the molecule, for steric reasons, there is an elongation of the Me2C-C(N)N bond to 1.603 (5) A degrees. The formation of dimers via N-H center dot center dot center dot O C hydrogen bonds with an interaction energy of 93.30 kJ mol(-1) and through cavities (33.7% of the unit-cell volume) was established in the packing of the molecules. There are no pi-stacking interactions in the structure.

Welcome to talk about 88-68-6, If you have any questions, you can contact Chernyshov, VV; Gatilov, YV; Yarovaya, OI; Koskin, IP; Yarovoy, SS; Brylev, KA; Salakhutdinov, NF or send Email.. Name: 2-Aminobenzamide

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

HPLC of Formula: C7H8N2O. Recently I am researching about MUTANT P53; CANCER-CELLS; CP-31398; RESEARCHES; GROWTH; IDENTIFICATION; INHIBITORS; BINDING; PROTEIN; TARGET, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [81960638, 21362007, 21462008]; Guangxi Natural Science FoundationNational Natural Science Foundation of Guangxi Province [2017GXNSFDA198045]; Foundation of State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Guangxi Normal University) [CMEMR2018-A1]; Innovation Project of Guangxi Graduate Education [YCBZ2018032, YCSW2017062]. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Wei, XW; Yuan, JM; Huang, WY; Chen, NY; Li, XJ; Pan, CX; Mo, DL; Su, GF. The CAS is 88-68-6. Through research, I have a further understanding and discovery of 2-Aminobenzamide

Forty-eight analogues of CP-31398, an antitumor agent modulated the mutant p53 gene were synthesized and their cytotoxicities against four cancer cell lines with different p-53 status including bladder cell 724 (w-p53), gastric cell MGC-803 (m-p53), prostate cell DU145 (m-p53), prostate cell PC-3 (null-p53), lung cell A549 (w-p53) and normal liver cell line HL-7702 (w-p53) were examined. (E)-2-(4-Nitrostyryl)-4-(3-dimethylaminopropyl)-aminoquinazoline (10ah) was identified as the most potent compound in anti-proliferation against MGC-803 cells, with IC50 lowed to 1.73 mu M, far potency than that of CP-31398. Molecular mechanism study revealed that 10ah and CP-31398 differ greatly in mechanism to exert their antitumor properties. 10ah could intercalate into DNA and resulted in significant DNA double-strand break 10ah-treatment in MGC-803 cells increased the expression of p53, phosphorylated p53 (p-p53), CDK4, p21 to cause cell cycle arrest at G2/M phase, significantly up-regulated the levels of pro-apoptosis proteins Bak, Bax, Bim while down-regulated the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclin B1, fluctuated the intracellular reactive oxygen species (ROS), Ca2+ and mitochondria! membrane potential, activated Caspase-9 and Caspase-3 to induce apoptosis. 10ah also displayed potent anticancer efficiency against MGC-803 xenograft tumors models, with tumor growth inhibition (TGI) up to 61.8% at 20 mg/kg without obvious toxicity. (C) 2019 Elsevier Masson SAS. All rights reserved.

HPLC of Formula: C7H8N2O. Welcome to talk about 88-68-6, If you have any questions, you can contact Wei, XW; Yuan, JM; Huang, WY; Chen, NY; Li, XJ; Pan, CX; Mo, DL; Su, GF or send Email.

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

In 2020 ACS OMEGA published article about ALDOSE REDUCTASE; DERIVATIVES; QUINAZOLINE-2,4(1H,3H)-DIONES; INHIBITORS; EFFICIENT; DESIGN; CO2; TRANSFORMATION; DISCOVERY; ARYLATION in [Li, Peng; Qin, Rongfei; Li, Gang; Huang, Haihong] Peking Union Med Coll & Chinese Acad Med Sci, Beijing Key Lab Act Subst Discovery & Druggabil E, Inst Mat Med, Beijing 100050, Peoples R China; [Li, Peng; Qin, Rongfei; Li, Gang; Huang, Haihong] Peking Union Med Coll & Chinese Acad Med Sci, Chinese Acad Med Sci, Key Lab AntiDR TB Innovat Drug Res, Inst Mat Med, Beijing 100050, Peoples R China; [Chen, Hui; Yan, Hong] Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing Key Lab Environm & Viral Oncol, Beijing 100124, Peoples R China in 2020, Cited 40. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6. HPLC of Formula: C7H8N2O

The one-pot synthesis of quinazoline-2,4-diones was developed in the presence of 4-dimethylaminopyridine (DMAP) by metal-free catalysis. The commercially available (Boc)(2)O acted as a key precursor in the construction of the 2-position carbonyl of quinazolinediones. The p-methoxybenzyl (PMB)-activated hetero- cyclization could smoothly proceed at room temperature instead of the microwave condition. This strategy is compatible with a variety of substrates with different functional groups. Furthermore, this protocol was utilized to smoothly prepare Zenarestat with a total yield of 70%.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

Meerakrishna, RS; Shanmugam, P in [Meerakrishna, Ramakrishnan Suseela; Shanmugam, Ponnusamy] CLRI, CSIR, Organ & Bioorgan Chem Div, Chennai 600020, Tamil Nadu, India published Synthesis of blue-red emissive amido-substituted di(het)aryl and tri(het)aryl amine derivatives via chemoselective N-mono and N,N-diarylation of (het) aryl amino amides using benzyne/arynes in 2019, Cited 48. COA of Formula: C7H8N2O. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6.

Herein, via chemoselective N-mono and N,N-diarylation of an aryl/hetaryl amino amide reaction using benzyne or arynes, an amide-substituted triaryl amine derivative and diaryl amine derivatives were afforded. The scope and limitation of the present study have been studied. The products thus obtained were synthetically transformed to highly functionalized biphenyl bridged heterocycles via Suzuki coupling and condensation with 4,4-biphenyl dialdehyde. Evaluation of the photophysical properties has revealed that the triaryl amine derivatives are blue emissive with high quantum yields, whereas the heterocyclic triaryl amine derivatives are blue-red emissive. The benzofuran-derived compound 4i was found to be blue emissive with high quantum yield, whereas the pyridine-derived compound 5j was found to be red emissive with low quantum yield.

Welcome to talk about 88-68-6, If you have any questions, you can contact Meerakrishna, RS; Shanmugam, P or send Email.. COA of Formula: C7H8N2O

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

An article Triazole-Based Inhibitors of the Wnt/beta-Catenin Signaling Pathway Improve Glucose and Lipid Metabolisms in Diet-Induced Obese Mice WOS:000457067600022 published article about BETA-CATENIN; NEGATIVE REGULATOR; WNT; TCF7L2; GENE; ACTIVATION; BINDING; RISK; SUSCEPTIBILITY; MECHANISMS in [Obianom, Obinna N.; Ai, Yong; Li, Yingjun; Yang, Wei; Guo, Dong; Yang, Hong; Xue, Fengtian; Shu, Yan] Univ Maryland, Sch Pharm, Dept Pharmacal Sci, Baltimore, MD 21201 USA; [Sakamuru, Srilatha; Xia, Menghang] NIH, Natl Ctr Adv Translat Sci, Bldg 10, Bethesda, MD 20892 USA; [Shu, Yan] Guangzhou Med Univ, Sch & Hosp Stomatol, Guangzhou 510140, Guangdong, Peoples R China; [Yang, Wei] Jiangsu Food & Pharmaceut Sci Coll, Pharmaceut Engn, Huaian 223005, Jiangsu, Peoples R China in 2019, Cited 51. Product Details of 88-68-6. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6

Wnt/beta-catenin signaling pathway is implicated in the etiology and progression of metabolic disorders. Although lines of genetic evidence suggest that blockage of this pathway yields favorable outcomes in treating such ailments, few inhibitors have been used to validate the promising genetic findings. Here, we synthesized and characterized a novel class of triazole-based Wnt/beta-catenin signaling inhibitors and assessed their effects on energy metabolism. One of the top inhibitors, compound 3a, promoted Axin stabilization, which led to the proteasome degradation of beta-catenin and subsequent inhibition of the Wnt/beta-catenin signaling in cells. Treatment of hepatocytes and high fat diet-fed mice with compound 3a resulted in significantly decreased hepatic lipid accumulation. Moreover, compound 3a improved glucose tolerance of high fat diet-fed mice without noticeable toxicity, while downregulating the genes involved in the glucose and fatty acid anabolisms. The new inhibitors are expected to be further developed for the treatment of metabolic disorders.

Welcome to talk about 88-68-6, If you have any questions, you can contact Obianom, ON; Ai, Y; Li, YJ; Yang, W; Guo, D; Yang, H; Sakamuru, S; Xia, MH; Xue, FT; Shu, Y or send Email.. SDS of cas: 88-68-6

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

An article N-donor 2-(Sulfonamido)benzamide ligands, their palladium(II) coordination species and C-C coupling catalysis efficiencies WOS:000487932000035 published article about SUZUKI-MIYAURA REACTION; PRE-CATALYSTS; COMPLEXES; ARYL; CHLORIDES; NANOPARTICLES; IMIDAZOLE; NICKEL; SERIES in [Oloyede, Hammed Olawale; Woods, Joseph Anthony Orighomisan] Univ Ibadan, Dept Chem, Inorgan Chem Unit, Ibadan, Nigeria; [Oloyede, Hammed Olawale; Goerls, Helmar; Plass, Winfried; Eseola, Abiodun Omokehinde] Friedrich Schiller Univ Jena, Inst Anorgan & Analyt Chem, Humboldtstr 8, D-07743 Jena, Germany; [Eseola, Abiodun Omokehinde] Redeemers Univ Ede, Dept Chem Sci, Mat Chem Grp, Ede, Osun State, Nigeria in 2019, Cited 51. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6. Product Details of 88-68-6

A series of synthetically accessible ligands based on new 2-(R-sulfonamido)benzamide have been prepared (R = methyl for H3M; R = 4-toly for H3T and T2CN; R = 2,4,6-triisopropylphenyl for H(3)iP and HiPCN). The R-substituents were selected to vary in sizes. Allowing ligand H(3)iP and palladium acetate to stand in solvent leads to self-assembly of the well-defined solvent- and stoichiometry-controlled tetranuclear or hexanuclear coordination macromolecules Pd-4(iP)(2) and (PdHiP)(6), which were analysed by X-ray crystallography. It was observed that palladium active species for Suzuki coupling catalysis could be stabilized by these simple and synthetically assessable N-donor ligands as revealed by turnover frequencies reaching 5500h(-1). Electronic features of these N-donors appear to be more important than the steric properties. (C) 2019 Elsevier B.V. All rights reserved.

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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem

An article Synthesis, Characterization and Antibacterial Evaluation of 2, 3Dihydroquinazolin-4 (1H)-Ones and Some New Bis 2, 3-Dihydroquinazolin-4 (1H)-Ones Using Pre-made Pyrazole Carbaldehyde Derivatives WOS:000631153800002 published article about GREEN SYNTHESIS; BIOLOGICAL EVALUATION; ASSISTED SYNTHESIS; EFFICIENT; CATALYST; 2,3-DIHYDROQUINAZOLIN-4(1H)-ONES; QUINAZOLINONES; FACILE in [Sina, Kiana Faraji; Yahyazadeh, Asieh; Mahmoodi, Nosrat Ollah] Univ Guilan, Fac Sci, Dept Chem, POB 41335-1914, Rasht, Iran in 2021, Cited 41. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6. Name: 2-Aminobenzamide

2, 3-Dihydroquinazolinones are of popular compounds with the diversification of biological and pharmacological activities. Among many discovered methods, there are efficient and convenient methods used for the synthesis of 2, 3-dihydroquinazoline-4 (1H)-one and some new bis 2, 3-dihydroquinazoline-4 (1H)-one derivatives which are reported in this study. The mentioned methods include the two-component condensation of one molecule of anthranilamide and one molecule of pyrazole carbaldehyde using montmorillonite-K 10 as a catalyst for the preparation of 2, 3 dihydroquinazoline-4 (1H)-ones. Also, one-pot pseudo-five-component reaction (5MCRs) of two molecules of isatoic anhydride, two molecules of pyrazole carbaldehydes and one molecule of ethan-1, 2-diamine in the presence of the r catalyst (montmorillonite-K10) for the synthesis of bis 2, 3-dihydroquinazoline-4 (1H)-ones. Despite the short times of reactions, high yields of products were obtained, which were validated using FT-IR, (HNMR)-H-1, (CNMR)-C-13, and elemental analysis. Moreover, the compounds were screened for their antimicrobial activities against two-gram-positive bacterial strains: Staphylococcus aureus and Micrococcus Luteus; and against two-gram-negative bacterial strains, as well: Escherichia coli and Pseudomonas aeruginosa, which all were utilized for antibacterial investigations. The results showed moderate or significant antibacterial activities.

Welcome to talk about 88-68-6, If you have any questions, you can contact Sina, KF; Yahyazadeh, A; Mahmoodi, NO or send Email.. Name: 2-Aminobenzamide

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

An article An anthranilamide-substituted borane [H-B(aam)]: its stability and application to iridium-catalyzed stereoselective hydroboration of alkynes WOS:000468369900026 published article about C-H BORYLATION; HETEROTOPIC OSSIFICATION; FORMAL HYDROBORATION; ITERATIVE SYNTHESIS; COUPLING MODULES; ARYL HALIDES; ACIDS; STRATEGY; HYDRIDE; VINYL in [Yoshida, Hiroto; Kimura, Miki; Tanaka, Hideya; Murashige, Yuya; Kageyuki, Ikuo; Osaka, Itaru] Hiroshima Univ, Grad Sch Engn, Dept Appl Chem, Higashihiroshima 7398527, Japan in 2019, Cited 38. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6. Product Details of 88-68-6

A new anthranilamide-substituted borane [H-B(aam)] was synthesized and found to serve as a stable, easy-to-handle substitute for H-B(pin). It was applied to the direct synthesis of diverse linear (E)-alkenyl-B(aam) s via regio-and stereoselective hydroboration of terminal alkynes under iridium catalysis. A boryliridium hydride complex arising from the oxidative addition of H-B(aam) to the Ir catalyst was isolated and characterized via NMR studies.

Product Details of 88-68-6. Welcome to talk about 88-68-6, If you have any questions, you can contact Yoshida, H; Kimura, M; Tanaka, H; Murashige, Y; Kageyuki, I; Osaka, I or send Email.

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

Authors Li, ED; Lin, Q; Meng, YQ; Zhang, LY; Song, PP; Li, N; Xin, JC; Yang, P; Bao, CN; Zhang, DQ; Zhang, Y; Wang, JK; Zhang, QR; Liu, HM in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER published article about BIOLOGICAL EVALUATION; DERIVATIVES; PI3K/AKT/MTOR; GEFITINIB; PATHWAY; DESIGN; GROWTH in [Li, Er-dong; Lin, Qiao; Meng, Ya-qi; Zhang, Lu-ye; Song, Pan-pan; Li, Na; Xin, Jing-chao; Yang, Peng; Bao, Chong-nan; Zhang, Dan-qing; Zhang, Yang; Wang, Ji-kuan; Zhang, Qiu-rong; Liu, Hong-min] Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Henan, Peoples R China; [Li, Er-dong; Lin, Qiao; Meng, Ya-qi; Zhang, Lu-ye; Song, Pan-pan; Li, Na; Xin, Jing-chao; Yang, Peng; Bao, Chong-nan; Zhang, Dan-qing; Zhang, Yang; Wang, Ji-kuan; Zhang, Qiu-rong; Liu, Hong-min] Collaborat Innovat Ctr New Drug Res & Safety Eval, Zhengzhou 450001, Henan, Peoples R China in 2019, Cited 32. Name: 2-Aminobenzamide. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6

A series of novel 2,4-disubstituted quinazolines were synthesized and evaluated for their anti-tumor activity against five human cancer cells (MDA-MB-231, MCF-7, PC-3, HGC-27 and MGC-803) using MIT assay. Among them, compound 9n showed the most potent cytotoxicity against breast cancer cells. Compound 9n also significantly inhibited the colony formation and migration of MDA-MB-231 and MCF-7 cells. Meanwhile, compound 9n induced cell cycle arrest at G1 phase and cell apoptosis, as well as increased accumulation of intracellular ROS. Furthermore, compound 9n exerted anti-tumor effects in vitro via decreasing the expression of anti-apoptotic protein Bcl-2 and increasing the pro-apoptotic protein Bax and p53. Mechanistically, compound 9n markedly decreased p-EGFR and p-PI3K expression, which revealed that compound 9n targeted breast cancer cells via interfering with EGFR-PI3K signaling pathway. Molecular docking suggested that compound 9n could indeed bind into the active pocket of EGFR. All the findings suggest that compound 9n might be a valuable lead compound for anti-tumor agents targeting breast cancer cells. (C) 2019 Elsevier Masson SAS. All rights reserved.

Name: 2-Aminobenzamide. Welcome to talk about 88-68-6, If you have any questions, you can contact Li, ED; Lin, Q; Meng, YQ; Zhang, LY; Song, PP; Li, N; Xin, JC; Yang, P; Bao, CN; Zhang, DQ; Zhang, Y; Wang, JK; Zhang, QR; Liu, HM or send Email.

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