Tag: M.W=100-150

Recently I am researching about PALLADIUM-CATALYZED ALKYLATION; THERMAL OXIDATIVE-DEGRADATION; POLYETHYLENE-GLYCOL; STEREOSELECTIVE-SYNTHESIS; SELECTIVE ALKYLATION; ALPHA-METHYLATION; C(SP(3))-H BONDS; METHANOL; ARYLACRYLAMIDES; HETEROCYCLES, Saw an article supported by the Ministry of Science and Technology (MOST), TaiwanMinistry of Science and Technology, Taiwan; Centre for Research and Development of Kaohsiung Medical University. Published in ROYAL SOC CHEMISTRY in CAMBRIDGE ,Authors: Kudale, VS; Wang, JJ. The CAS is 88-68-6. Through research, I have a further understanding and discovery of 2-Aminobenzamide. Name: 2-Aminobenzamide

The generation of a methyl carbon source from renewable and cheap sources is challenging. Herein, we describe a novel and an efficient route for methylation and acetylation of aza-heteroarenes using PEG-400 under O-2 and TsOH center dot H2O for the first time by tuning the reaction conditions using a different set of starting materials. The key features of the current protocol are oxidative C-O and C-C bond scission under metal-free conditions with good functional group tolerance, and a broad substrate scope. The potential applicability of the designed methodology was demonstrated for the synthesis of central nervous system (CNS) depressant and anticonvulsant drug molecules by a one-pot strategy.

About 2-Aminobenzamide, If you have any questions, you can contact Kudale, VS; Wang, JJ or concate me.. Name: 2-Aminobenzamide

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

COA of Formula: C7H8N2O. Recently I am researching about C/EBP-ALPHA; INHIBITORS; CYTOTOXICITY; CANCER, Saw an article supported by the Singapore Ministry of Health’s National Medical Research Council under its Singapore Translational Research (STaR) Investigator AwardMinistry of Health-SingaporeNational Medical Research Council, Singapore; National Research Foundation SingaporeNational Research Foundation, Singapore; Singapore Ministry of Education under its Research Centres of Excellence initiativeMinistry of Education, Singapore; Cancer Science Institute of Singapore; National Institution of HealthUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USA [P01 CA66996, R21CA178301, R01CA169259]; American Cancer SocietyAmerican Cancer Society [RSG-13-047]; Harvard Stem Cell Institute Blood Program [DP-0110-12-00]; CSIR-HRDGCouncil of Scientific & Industrial Research (CSIR) – India [13(8906-A)/2017-pool]; CSIR, New DelhiCouncil of Scientific & Industrial Research (CSIR) – India [CSC0301]. Published in PERGAMON-ELSEVIER SCIENCE LTD in OXFORD ,Authors: Radhakrishnan, S; Syed, R; Takei, H; Kobayashi, IS; Nakamura, E; Sultana, F; Kamal, A; Tenen, DG; Kobayashi, SS. The CAS is 88-68-6. Through research, I have a further understanding and discovery of 2-Aminobenzamide

The tumor suppressor transcription factor CCAAT enhancer-binding protein alpha (C/EBP alpha) expression is down-regulated in myeloid leukemias and enhancement of C/EBP alpha expression induces granulocytic differentiation in leukemic cells. Previously we reported that Styryl quinazolinones induce myeloid differentiation in HL-60 cells by upregulating C/EBP alpha expression. To identify more potent molecule that can induce leukemic cell differentiation we synthesized and evaluated new series of styryl quinazolinones, ethynyl styryl quinazolinones, styryl quinolinones and thienopyrimidinones. Thienopyrimidinones were found toxic and styryl quinolinones were found inactive. Ethynyl styryl quinazolinone 39 and styryl quinazolinone 5 were found active on par with the earlier reported analogues 1 and 2 suggesting that the 5-nitro furan-2-yl styryl quinazolinones find a real promise in leukemic cell differentiation. The improved potency of 5 suggested that further modifications in the 5-nitro furan-2-yl styryl quinazolinones can be at the phenyl substitution at the 3-position of the quinazolinone ring apart from the 5-position of the heteroaryl ring.

COA of Formula: C7H8N2O. About 2-Aminobenzamide, If you have any questions, you can contact Radhakrishnan, S; Syed, R; Takei, H; Kobayashi, IS; Nakamura, E; Sultana, F; Kamal, A; Tenen, DG; Kobayashi, SS or concate me.

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

Chernyshov, VV; Gatilov, YV; Yarovaya, OI; Koskin, IP; Yarovoy, SS; Brylev, KA; Salakhutdinov, NF in [Chernyshov, Vladimir V.; Gatilov, Yuri, V; Yarovaya, Olga, I; Koskin, Igor P.; Salakhutdinov, Nariman F.] NN Vorozhtsov Novosibirsk Inst Organ Chem SB RAS, 9 Acad Lavrentiev Ave, Novosibirsk 630090, Russia; [Chernyshov, Vladimir V.; Gatilov, Yuri, V; Yarovaya, Olga, I; Brylev, Konstantin A.] Novosibirsk State Univ, Pirogova St 2, Novosibirsk 630090, Russia; [Yarovoy, Spartak S.; Brylev, Konstantin A.] Nikolaey Inst Inorgan Chem SB RAS, 3 Acad Lavrentiev Ave, Novosibirsk 630090, Russia published The first example of the stereoselective synthesis and crystal structure of a spirobicycloquinazolinone based on (-)-fenchone and anthranilamide in 2019, Cited 41. Category: thiomorpholine. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6.

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.

Category: thiomorpholine. About 2-Aminobenzamide, If you have any questions, you can contact Chernyshov, VV; Gatilov, YV; Yarovaya, OI; Koskin, IP; Yarovoy, SS; Brylev, KA; Salakhutdinov, NF or concate me.

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

I found the field of Chemistry very interesting. Saw the article Photocatalyst-free visible-light-promoted quinazolinone synthesis at room temperature utilizing aldehydes generated in situ via C=C bond cleavage published in 2021. Category: thiomorpholine, Reprint Addresses Xie, ZB; Le, ZG (corresponding author), East China Univ Technol, Jiangxi Prov Key Lab Synthet Chem, Nanchang 330013, Jiangxi, Peoples R China.; Xie, ZB; Le, ZG (corresponding author), East China Univ Technol, Sch Chem Biol & Mat Sci, Nanchang 330013, Jiangxi, Peoples R China.. 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.

Category: thiomorpholine. About 2-Aminobenzamide, If you have any questions, you can contact Xie, ZB; Lan, J; Yan, LY; Chen, XH; Li, Q; Meng, J; Le, ZG or concate me.

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

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. COA 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.

COA of Formula: C7H8N2O. About 2-Aminobenzamide, If you have any questions, you can contact Sonawane, VR; Siddique, MUM; Gatchie, L; Williams, IS; Bharate, SB; Jayaprakash, V; Sinha, BN; Chaudhuri, B or concate me.

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

An article Anthranilamide (aam)-substituted arylboranes in direct carbon-carbon bond-forming reactions WOS:000459737100006 published article about CROSS-COUPLING REACTION; BORONIC ACIDS; FORMAL HYDROBORATION; CATALYZED BORYLATION; ITERATIVE SYNTHESIS; GENERAL-SOLUTION; COPPER; ALKYNES; ARYL; STRATEGY in [Kamio, Shintaro; Kageyuki, Ikuo; Osaka, Itaru; Yoshida, Hiroto] Hiroshima Univ, Grad Sch Engn, Dept Appl Chem, Higashihiroshima 7398527, Japan in 2019, Cited 34. HPLC of Formula: C7H8N2O. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6

Anthranilamide (aam)-substituted arylboranes, which were reported to serve as masked boranes in the Suzuki-Miyaura coupling, have been found to be directly cross-coupled just by use of an aqueous medium. The excellent stability of 2-pyridyl-B(aam) toward protodeborylation allowed their smooth cross-coupling.

About 2-Aminobenzamide, If you have any questions, you can contact Kamio, S; Kageyuki, I; Osaka, I; Yoshida, H or concate me.. HPLC of Formula: C7H8N2O

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

SDS of cas: 64-10-8. Martini, G; Cardone, C; Vitiello, PP; Belli, V; Napolitano, S; Troiani, T; Ciardiello, D; Della Corte, CM; Morgillo, F; Matrone, N; Sforza, V; Papaccio, G; Desiderio, V; Paul, MC; Moreno-Viedma, V; Normanno, N; Rachiglio, AM; Tirino, V; Maiello, E; Latiano, TP; Rizzi, D; Signoriello, G; Sibilia, M; Ciardiello, F; Martinelli, E in [Martini, Giulia; Cardone, Claudia; Vitiello, Pietro Paolo; Belli, Valentina; Napolitano, Stefania; Troiani, Teresa; Ciardiello, Davide; Della Corte, Carminia Maria; Morgillo, Floriana; Matrone, Nunzia; Ciardiello, Fortunato; Martinelli, Erika] Univ Campania L Vanvitelli, Med Oncol, Dept Precis Med, Via Pansini 5, I-80131 Naples, Italy; [Sforza, Vincenzo] Fdn Pascale, IRCCS, Ist Nazl Tumori, Dept Clin Expt Thorac Oncol, Naples, Italy; [Papaccio, Gianpaolo; Desiderio, Vincenzo; Tirino, Virginia] Univ Campania Luigi Vanvitelli Napoli, Dept Expt Med, Naples, Italy; [Paul, Mariel C.; Moreno-Viedma, Veronica; Sibilia, Maria] Med Univ Vienna, Comprehens Canc Ctr, Dept Med 1, Inst Canc Res, Borschkegasse 8a, Vienna, Austria; [Normanno, Nicola; Rachiglio, Anna Maria] Fdn Pascale, IRCCS, Ist Nazl Tumori, Cell Biol & Biotherapy Unit, Naples, Italy; [Maiello, Evaristo; Latiano, Tiziana Pia; Rizzi, Daniele] Hosp Casa Sollievo Della Sofferenza San Giovanni, Med Oncol, San Giovanni Rotondo, Italy; [Signoriello, Giuseppe] Univ Campania L Vanvitelli, Biostat, Dipartimento Salute Mentale & Fis & Med Prevent, Naples, Italy published EPHA2 Is a Predictive Biomarker of Resistance and a Potential Therapeutic Target for Improving Antiepidermal Growth Factor Receptor Therapy in Colorectal Cancer in 2019.0, Cited 24.0. The Name is 1-Phenylurea. Through research, I have a further understanding and discovery of 64-10-8.

The EPHA2 tyrosine kinase receptor is implicated in tumor progression and targeted therapies resistance. We evaluated EPHA2 as a potential resistance marker to the antiepidermal growth factor receptor (EGFR) monoclonal antibody cetuximab in colorectal cancer. We studied activation of EPHA2 in a panel of human colorectal cancer cell lines sensitive or resistant to anti-EGFR drugs. The in vitro and in vivo effects of ALW-II-41-27 (an EPHA2 inhibitor) and/or cetuximab treatment were tested. Fonnalin-fixed paraffin-embedded tumor specimens from 82 RAS wild-type (WV) metastatic colorectal cancer patients treated with FOLFIRI + cetuximab as first-line therapy in the CAPRI-COIM trial were assessed for EPHA2 expression by immunohistochemistry and correlated with treatment efficacy. EPHA2 was differentially activated in colorectal cancer cell lines. Combined treatment with ALW-II-41-27 plus cetuximab reverted primary and acquired resistance to cetuximab, causing cell growth inhibition, inducing apoptosis and cell-cycle G1-G2 arrest. In tumor xenograft models, upon progression to cetuximab, ALW-II-41-27 addition significantly inhibited tumor growth. EPHA2 protein expression was detected in 55 of 82 tumor samples, frequently expressed in less-differentiated and left-sided tumors. High levels of EPHA2 significantly correlated with worse progression-free survival [8.6 months; confidence interval (CI) 95%, 6.4-10.8; vs. 12.3 months; CI 95%, 10.4-14,2; P = 0.03] and with increased progression rate (29% vs. 9%, P = 0.02). A specific EPHA2 inhibitor reverts in vitro and in vivo primary and acquired resistance to anti-ECFR therapy. EPHA2 levels are significantly associated with worse outcome in patients treated with FOLFIRI + cetuximab. These results highlight EPHA2 as a potential therapeutic target in metastatic colorectal cancer.

About 1-Phenylurea, If you have any questions, you can contact Martini, G; Cardone, C; Vitiello, PP; Belli, V; Napolitano, S; Troiani, T; Ciardiello, D; Della Corte, CM; Morgillo, F; Matrone, N; Sforza, V; Papaccio, G; Desiderio, V; Paul, MC; Moreno-Viedma, V; Normanno, N; Rachiglio, AM; Tirino, V; Maiello, E; Latiano, TP; Rizzi, D; Signoriello, G; Sibilia, M; Ciardiello, F; Martinelli, E or concate me.. SDS of cas: 64-10-8

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

HPLC of Formula: C7H8N2O. Authors Yang, L; Hou, HQ; Li, L; Wang, J; Zhou, SY; Wu, M; Ke, F in ROYAL SOC CHEMISTRY published article about in [Yang, Li; Li, Lan; Ke, Fang] Yibin Univ, Coll Chem & Chem Engn, Yibin, Sichuan, Peoples R China; [Hou, Huiqing; Wang, Jin; Zhou, Sunying; Wu, Mei; Ke, Fang] Fujian Med Univ, Fuzhou, Fujian, Peoples R China in 2021, Cited 64. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6

An efficient and practical electrochemically catalyzed transition metal-free process for the synthesis of substituted quinazolinones from simple and readily available o-aminobenzonitriles and aldehydes in water has been accomplished. I-2/base and water play an unprecedented and vital role in the reaction. By electrochemically catalysed hydrolysis of o-aminobenzonitriles, the synthesis of quinazolinones with benzaldehyde was first proposed. The synthetic utility of this method was demonstrated by gram-scale operation, as well as the preparation of bioactive N-(2,5-dichlorophenyl)-6-(2,2,2-trifluoroethoxy) pteridin-4-amine, which enables straightforward, practical and environmentally benign quinazolinone formation.

About 2-Aminobenzamide, If you have any questions, you can contact Yang, L; Hou, HQ; Li, L; Wang, J; Zhou, SY; Wu, M; Ke, F or concate me.. HPLC of Formula: C7H8N2O

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

Krapf, MK; Gallus, J; Spindler, A; Wiese, M in [Krapf, Michael K.; Gallus, Jennifer; Spindler, Anna; Wiese, Michael] Univ Bonn, Inst Pharmaceut, Immenburg 4, D-53121 Bonn, Germany published Synthesis and biological evaluation of quinazoline derivatives – A SAR study of novel inhibitors of ABCG2 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.

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,

Product Details of 88-68-6. 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

I found the field of Chemistry; Computer Science; Environmental Sciences & Ecology; Mathematical & Computational Biology; Toxicology very interesting. Saw the article QSPR modelling of the soil sorption coefficient from training sets of different sizes published in 2019.0. Formula: C7H8N2O, Reprint Addresses Olguin, CJM (corresponding author), Western Parana State Univ, Grad Program Agr Engn PGEAGRI, Agroenvironm Sci Res Grp, Cascavel, Parana, Brazil.. The CAS is 64-10-8. Through research, I have a further understanding and discovery of 1-Phenylurea

Quantitative structure-property relationship (QSPR) modelling has been used in many scientific fields. This approach has been extensively applied in environmental research to predict physicochemical properties of compounds with potential environmental impact. The soil sorption coefficient is an important parameter for the evaluation of environmental risks, and it helps to determine the final fate of substances in the environment. In the last few years, different QSPR models have been developed for the determination of the sorption coefficient. In this study, several QSPR models were generated and evaluated for the prediction of log K-oc from the relationship with log P. These models were obtained from an extensive and diverse training set (n = 639) and from subsets of this initial set (i.e. halves, fourths and eighths). The aim of this study was to investigate whether the size of the training set affects the statistical quality of the obtained models. Furthermore, statistical equivalence was verified between the models obtained from smaller sets and the model obtained from the total training set. The results confirmed the equivalence between the models, thus indicating the possibility of using smaller training sets without compromising the statistical quality and predictive capability, as long as most chemical classes in the test set are represented in the training set.

Formula: C7H8N2O. About 1-Phenylurea, If you have any questions, you can contact Olguin, CJM; Sampaio, SC; dos Reis, RR; Remor, MB; Olguin, CFA or concate me.

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