Month: November 2021

In 2021 EUR J MED CHEM published article about VIRUS; ZANAMIVIR; EPIDEMIOLOGY; DERIVATIVES; RESISTANCE in [Zhao, Hongqian; Jiang, Siyuan; Ye, Zhifan; Zhu, Hongxi; Meng, Peipei; Wang, Kuanglei; Tian, Yongshou] Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Key Lab Struct Based Drug Design & Discovery, Minist Educ, 103 Wenhua Rd, Shenyang 110016, Peoples R China; [Hu, Baichun] Shenyang Pharmaceut Univ, Sch Pharm, 103 Wenhua Rd, Shenyang 110016, Peoples R China; [Zhang, Huicong] Shenyang Pharmaceut Univ, Wuya Coll Innovat, 103 Wenhua Rd, Shenyang 110016, Peoples R China; [Hu, Yanmei; Wang, Jun] Univ Arizona, Coll Pharm, Dept Pharmacol & Toxicol, Tucson, AZ 85721 USA in 2021, Cited 41. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5. SDS of cas: 123-11-5

Neuraminidase (NA) inhibitors play a prime role in treating influenza. However, a variety of viruses containing mutant NAs have developed severe drug resistance towards NA inhibitors, so it is of crucial significance to solve this problem. Encouraged by urea-containing compound 12 disclosed by our lab, we designed a series of oseltamivir derivatives bearing hydrazide fragment for targeting the 150 cavity. Among the synthesized compounds, compound 17a showed 8.77-fold, 4.12-fold, 203-fold and 6.23-fold more potent activity than oseltamivir carboxylate against NAs from H5N1, H1N1, H5N1-H274Y, H1N1-H274Y, respectively. Meanwhile, the best compound 17a exhibited satisfactory metabolic stability in vitro. This study offers an important reference for the structural optimization of oseltamivir aiming at potent inhibition against H274Y mutant of NAs. (C) 2021 Elsevier Masson SAS. All rights reserved.

SDS of cas: 123-11-5. Welcome to talk about 123-11-5, If you have any questions, you can contact Zhao, HQ; Jiang, SY; Ye, ZF; Zhu, HX; Hu, BC; Meng, PP; Hu, YM; Zhang, HC; Wang, KL; Wang, J; Tian, YS or send Email.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Recently I am researching about AGENTS; 4-THIAZOLIDINONES; ANALOGS; THIAZOLIDIN-4-ONE; CYTOTOXICITY; MICROTUBULES; POTENT; QSAR, Saw an article supported by the Department of Pharmaceuticals (DoP), Ministry of Chemicals & Fertilizers, Govt. of India, New Delhi,. Product Details of 120-14-9. Published in ELSEVIER in AMSTERDAM ,Authors: Sigalapalli, DK; Pooladanda, V; Kadagathur, M; Guggilapu, SD; Uppu, JL; Godugu, C; Bathini, NB; Tangellamudi, ND. The CAS is 120-14-9. Through research, I have a further understanding and discovery of 3,4-Dimethoxybenzaldehyde

Here-in, we present molecular design, chemical synthesis and evaluation of novel chromenyl-based 2-iminothiazolidin-4-one derivatives as tubulin polymerization inhibitors. The newly synthesized compounds were evaluated for their in vitro cytotoxicities against A549 (lung cancer), MDA-MB-231 and BT-471 (breast cancer), HepG2 (liver cancer) and HCT-116 (colon cancer) cell lines by MTT assay. Among the synthesized compounds, compound 12b showed excellent anticancer activity on MDA-MB-231 cell line with IC50 value of 0.95 +/- 1.88 mu M and was verified to be safe in normal human bronchial epithelial cells (Beas-2B). Apoptosis induced by the lead 12b was observed using morphological observations, AO/EB and DAPI staining procedures. Further, dose-dependent increase in the depolarization of mitochondrial membrane was also observed through JC-1 staining. Annexin V-FITC/PI assay confirmed that 12b induced early apoptosis. Additionally, cell cycle analysis indicated that the MDA-MB-231 cells were arrested at sub-G2/M phase and also inhibited tubulin polymerization with IC50 value of 3.54 +/- 0.2 mM. Molecular docking simulations were employed to identify the important binding modes responsible for the tubulin inhibitory activity, thus supporting their effective anticancer potential. (c) 2020 Published by Elsevier B.V.

Product Details of 120-14-9. Welcome to talk about 120-14-9, If you have any questions, you can contact Sigalapalli, DK; Pooladanda, V; Kadagathur, M; Guggilapu, SD; Uppu, JL; Godugu, C; Bathini, NB; Tangellamudi, ND or send Email.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

An article Discovery of Coumarin as Microtubule Affinity-Regulating Kinase 4 Inhibitor That Sensitize Hepatocellular Carcinoma to Paclitaxel WOS:000468900100001 published article about BIOLOGICAL EVALUATION; MARK4; TARGET; PROLIFERATION; CONDENSATION; CHECKPOINT; COMPLEX; DESIGN; FAMILY; GENE in [Shen, Xianyan; Liu, Xuesha; Wan, Shunli; Wang, Chun] Chinese Acad Sci, Chengdu Inst Biol, Chengdu, Sichuan, Peoples R China; [Liu, Xuesha; Fan, Xin; He, Huaiyu; Wei, Rong; Pu, Wenchen; Peng, Yong] West China Hosp, State Key Lab Biotherapy, Chengdu, Sichuan, Peoples R China; [Liu, Xuesha; Fan, Xin; He, Huaiyu; Wei, Rong; Pu, Wenchen; Peng, Yong] West China Hosp, Canc Ctr, Chengdu, Sichuan, Peoples R China; [Liu, Xuesha; Fan, Xin; He, Huaiyu; Wei, Rong; Pu, Wenchen; Peng, Yong] Sichuan Univ, Coll Life Sci, Chengdu, Sichuan, Peoples R China; [Liu, Xuesha; Fan, Xin; He, Huaiyu; Wei, Rong; Pu, Wenchen; Peng, Yong] Collaborat Innovat Ctr Biotherapy, Chengdu, Sichuan, Peoples R China in 2019.0, Cited 55.0. HPLC of Formula: C7H8O2. The Name is m-Methoxyphenol. Through research, I have a further understanding and discovery of 150-19-6

Hepatocellular carcinoma (HCC) is one of the most prevalent cancers worldwide. Nowadays, pharmacological therapy for HCC is in urgent needs. Paclitaxel is an effective drug against diverse solid tumors, but commonly resisted in HCC patients. We recently have disclosed that microtubule affinity-regulating kinase 4 (MARK4) increases the microtubule dynamics and confers paclitaxel resistance in HCC, suggesting MARK4 as an attractive target to overcome paclitaxel resistance. Herein, we synthesized and identified coumarin derivatives 50 as a novel MARK4 inhibitor. Biological evaluation indicated compound 50 directly interacted with MARK4 and inhibited its activity in vitro, suppressed cell viability and induced apoptosis of HCC cells in a MARK4-dependent manner. Importantly, compound 50 significantly increased the drug response of paclitaxel treatment to HCC cells, providing a promise strategy to HCC treatment and broadening the application of paclitaxel in cancer therapy.

Bye, fridends, I hope you can learn more about C7H8O2, If you have any questions, you can browse other blog as well. See you lster.. HPLC of Formula: C7H8O2

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Safety of m-Methoxyphenol. Carreras, L; Franconetti, A; Grabulosa, A; Frontera, A; Vidal-Ferran, A in [Carreras, Lucas; Vidal-Ferran, Anton] Inst Chem Res Catalonia ICIQ, Av Paisos Catalans 16, Tarragona 43007, Spain; [Franconetti, Antonio; Frontera, Antonio] Univ Illes Balears, Dept Quim, Crta Valldemossa Km 7-5, Palma De Mallorca 07122, Spain; [Grabulosa, Arnald; Vidal-Ferran, Anton] Univ Barcelona, Dept Inorgan & Organ Chem, Sect Inorgan Chem, Carrer Marti i Franques 1-11, Barcelona 08028, Spain; [Vidal-Ferran, Anton] ICREA, Pg Lluis Co 23, Barcelona 08010, Spain published Selective functionalisation of aromatic alcohols with supramolecularly regulated gold(i) catalysts in 2020.0, Cited 64.0. The Name is m-Methoxyphenol. Through research, I have a further understanding and discovery of 150-19-6.

Phosphite-based Au(i) catalytic systems containing an array of structurally diverse polyether-based regulation sites were designed and synthesised. These catalysts have been successfully tested in the Au(i)-catalysed C-H functionalisation of phenols and related derivatives with gold-carbenes derived from diazo compounds. Regulation of the steric congestion around the catalytic Au(i) centreviaion-dipole interactions with an external regulation agent led to an enhancement of both the activity and selectivity of the reaction. This new approach in supramolecular gold(i) catalysis has been applied to the derivatisation of an array of substituted phenols and related substrates and to the preparation of an advanced synthetic intermediate of the anticancer agent tamoxifen. The effects of the regulation agent on the selectivity and yield of the reaction have been studied and rationalised using DFT-D calculations.

Welcome to talk about 150-19-6, If you have any questions, you can contact Carreras, L; Franconetti, A; Grabulosa, A; Frontera, A; Vidal-Ferran, A or send Email.. Safety of m-Methoxyphenol

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Application In Synthesis of Mequinol. Authors Nakayama, Y; Maser, MR; Okita, T; Dubrovskiy, AV; Campbell, TL; Reisman, SE in AMER CHEMICAL SOC published article about in [Nakayama, Yasuaki; Maser, Michael R.; Okita, Tatsuya; Dubrovskiy, Anton, V; Campbell, Taryn L.; Reisman, Sarah E.] CALTECH, Warren & Katharine Schlinger Lab Chem & Chem Engn, Div Chem & Chem Engn, Pasadena, CA 91125 USA in 2021.0, Cited 38.0. The Name is Mequinol. Through research, I have a further understanding and discovery of 150-76-5

The first total synthesis of the cytotoxic alkaloid ritterazine B is reported. The synthesis features a unified approach to both steroid subunits, employing a titanium-mediated propargylation reaction to achieve divergence from a common precursor. Other key steps include gold-catalyzed cycloisomerizations that install both spiroketals and late stage C-H oxidation to incorporate the C7′ alcohol.

Application In Synthesis of Mequinol. About Mequinol, If you have any questions, you can contact Nakayama, Y; Maser, MR; Okita, T; Dubrovskiy, AV; Campbell, TL; Reisman, SE or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Name: Benzyl Alcohol. In 2020.0 ORG LETT published article about ASYMMETRIC TRANSFER HYDROGENATION; RUTHENIUM COMPLEXES; EFFICIENT CATALYST; CARBOXYLIC-ACIDS; KETONES; REDUCTION; CARBONYL; IRON; ALDEHYDES; HYDROSILATION in [Behera, Rakesh R.; Ghosh, Rahul; Panda, Surajit; Khamari, Subrat; Bagh, Bidraha] HBNI, NISER, Sch Chem Sci, Bhubaneswar 752050, Odisha, India in 2020.0, Cited 109.0. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6.

Selective and efficient hydrosilylations of esters to alcohols by a well-defined manganese(I) complex with a commercially available bisphosphine ligand are described. These reactions are easy alternatives for stoichiometric hydride reduction or hydrogenation, and employing cheap, abundant, and nonprecious metal is attractive. The hydrosilylations were performed at 100 degrees C under solvent-free conditions with low catalyst loading. A large variety of aromatic, aliphatic, and cyclic esters bearing different functional groups were selectively converted into the corresponding alcohols in good yields.

Name: Benzyl Alcohol. Bye, fridends, I hope you can learn more about C7H8O, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

HPLC of Formula: C9H7NO2. Authors Chheda, PR; Kummer, DA; Nishimura, RT; McClure, KJ; Venkatesan, H in AMER CHEMICAL SOC published article about in [Kummer, David A.] Lundbeck La Jolla Res Ctr Inc, San Diego, CA 92121 USA; [Chheda, Pratik R.; Nishimura, Rachel T.; McClure, Kelly J.; Venkatesan, Hariharan] Janssen Res & Dev, Discovery Chem, San Diego, CA 92121 USA in 2021, Cited 63. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3

A one-pot, Hantzsch ester-mediated Knoevenagel condensation-reduction reaction has been developed for alkylation of a wide range of substituted 2,4-quinoline diols and 2,4-pyridine diols with aldehydes. The process is operationally simple to perform, scalable, and provides highly useful C-3 alkylated quinoline and pyridine diols in yields of 58-92%. The alkylation products can be converted to 2,4-dihaloquinoline and pyridine substrates for further functionalization.

HPLC of Formula: C9H7NO2. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Chheda, PR; Kummer, DA; Nishimura, RT; McClure, KJ; Venkatesan, H or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

An article Chromium-Salen Complex/Nitroxyl Radical Cooperative Catalysis: A Combination for Aerobic Intramolecular Dearomative Coupling of Phenols WOS:000649101400083 published article about OXIDATION; ALCOHOLS; DERIVATIVES; COMPLEXES; MORPHINE in [Nagasawa, Shota; Fujiki, Shogo; Sasano, Yusuke; Iwabuchi, Yoshiharu] Tohoku Univ, Grad Sch Pharmaceut Sci, Aoba Ku, Sendai, Miyagi 9808578, Japan in 2021.0, Cited 48.0. Computed Properties of C8H8O2. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5

We describe an aerobic intramolecular dearomative coupling reaction of tethered phenols using a catalytic system consisting of a chromium-salen (Cr-salen) complex combined with a nitroxyl radical. This novel catalytic system enables formation of various spirocyclic dienone products including those unable to be accessed by previously reported methods efficiently under mild reaction conditions.

Welcome to talk about 123-11-5, If you have any questions, you can contact Nagasawa, S; Fujiki, S; Sasano, Y; Iwabuchi, Y or send Email.. Computed Properties of C8H8O2

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

I found the field of Pharmacology & Pharmacy very interesting. Saw the article Discovery and Biological Evaluation of N-Methyl-pyrrolo[2,3-b]pyridine-5-carboxamide Derivatives as JAK1-Selective Inhibitors published in 2021. Application In Synthesis of 4-Methoxybenzaldehyde, Reprint Addresses Kang, S (corresponding author), Ewha Womans Univ, Coll Pharm, Seoul 03760, South Korea.; Kang, S (corresponding author), Ewha Womans Univ, Grad Sch Pharmaceut Sci, Seoul 03760, South Korea.. The CAS is 123-11-5. Through research, I have a further understanding and discovery of 4-Methoxybenzaldehyde

Janus kinase 1 (JAK1) plays a key role in most cytokine-mediated inflammatory and autoimmune responses through JAK/STAT signaling; thus, JAK1 inhibition is a promising therapeutic strategy for several diseases. Analysis of the binding modes of current JAK inhibitors to JAK isoforms allowed the design of N-alkyl-substituted 1-H-pyrrolo[2,3-b] pyridine carboxamide as a JAK1-selective scaffold, and the synthesis of various methyl amide derivatives provided 4- ((cis-1- (4-chlorobenzyl)-2-methylpiperidin-4-yl) amino-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide (31g) as a potent JAK1-selective inhibitor. In particular, the (S,S)-enantiomer of 31g (38a) exhibited excellent potency for JAK1 and selectivity over JAK2, JAK3, and TYK2. On investigating the effect of 31g on hepatic fibrosis, it was found that it reduces the proliferation and fibrogenic gene expression of TGF-beta-induced hepatic stellate cells (HSCs). Specifically, 31g significantly inhibited TGF-beta-induced migration of HSCs at 0.25 mu M in wound-healing assays.

Bye, fridends, I hope you can learn more about C8H8O2, If you have any questions, you can browse other blog as well. See you lster.. Application In Synthesis of 4-Methoxybenzaldehyde

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

HPLC of Formula: C7H8O. Authors Trewhela, T; Ancey, C; Gray, JMNT in CAMBRIDGE UNIV PRESS published article about in [Trewhela, T.; Ancey, C.] Ecole Polytech Fed Lausanne, CH-1015 Lausanne, Switzerland; [Gray, J. M. N. T.] Univ Manchester, Dept Math, Oxford Rd, Manchester M13 9PL, Lancs, England; [Gray, J. M. N. T.] Univ Manchester, Manchester Ctr Nonlinear Dynam, Oxford Rd, Manchester M13 9PL, Lancs, England in 2021.0, Cited 68.0. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6

Particles of differing sizes are notoriously prone to segregation in shear driven flows under the action of gravity. This has important implications in many industrial processes, where particle-size segregation can lead to flow problems and reduced product quality, as well as longer product development and start-up times. Particle-size segregation also readily occurs in many hazardous geophysical mass flows (such as snow avalanches, debris flows and volcanic pyroclastic flows) and can lead to the formation of destructive bouldery flow fronts and significantly longer runouts. Although general theories exist to model particle-size segregation, the detailed functional dependence of the segregation flux on the shear rate, gravity, pressure, particle concentration, grain size and grain-size ratio is still not known. This paper describes refractive-index matched oscillatory shear-cell experiments that shed light on the segregation velocity in the two extreme cases of (i) a single large intruder rising up through a matrix of smaller grains, and (ii) a single small intruder percolating down through a matrix of large particles. Despite the sometimes markedly different time scales for segregation in these two situations, a unifying scaling law has been found that is able to collapse all the experimental data over a wide range of shear rates and grain-size ratios in the range . The resulting functional form is easily generalizable to intermediate concentrations and can quantitatively capture laboratory experiments and numerical simulations with a mix of large and small grains.

Welcome to talk about 100-51-6, If you have any questions, you can contact Trewhela, T; Ancey, C; Gray, JMNT or send Email.. HPLC of Formula: C7H8O

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles