Day: October 9, 2021

In 2019 ACS MED CHEM LETT published article about MULTIKINASE INHIBITOR; DISCOVERY; RESISTANCE; SORAFENIB; MUTATIONS; PATHWAY in [Assadieskandar, Amir; Yu, Caiqun; Zhang, Chao] Univ Southern Calif, Loker Hydrocarbon Res Inst, Los Angeles, CA 90089 USA; [Assadieskandar, Amir; Yu, Caiqun; Zhang, Chao] Univ Southern Calif, Dept Chem, Los Angeles, CA 90089 USA; [Zhang, Chao] Univ Southern Calif, USG Norris Comprehens Canc Ctr, Los Angeles, CA 90089 USA; [Maisonneuve, Pierre; Sicheri, Frank] Sinai Hlth Syst, Lunenfeld Tanenbaum Res Inst, Toronto, ON M5G 1X5, Canada; [Sicheri, Frank] Univ Toronto, Dept Mol Genet, Toronto, ON, Canada; [Sicheri, Frank] Univ Toronto, Dept Biochem, Toronto, ON, Canada; [Kunnov, Igor] Cornell Univ, NE CAT, Dept Chem & Chem Biol, Argonne, IL 60439 USA in 2019, Cited 24. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9. Quality Control of 3-(Trifluoromethyl)phenol

One effective means to achieve inhibitor specificity for RAF kinases, an important family of cancer drug targets, has been to target the monomeric inactive state conformation of the kinase domain, which, unlike most other kinases, can accommodate sulfonamide-containing drugs such as vemurafenib and dabrafenib because of the presence of a unique pocket specific to inactive RAF kinases. We previously reported an alternate strategy whereby rigidification of a nonselective pyrazolo[3,4-d]pyrimidine-based inhibitor through ring closure afforded moderate but appreciable increases in selectivity for RAF kinases. Here, we show that a further application of the rigidification strategy to a different pyrazolopyrimidine-based scaffold dramatically improved selectivity for RAF kinases. Crystal structure analysis confirmed our inhibitor design hypothesis revealing that 21 engages an active-like state conformation of BRAF normally associated with poorly discriminating inhibitors. When screened against a panel of distinct cancer cell lines, the optimized inhibitor 21 primarily inhibited the proliferation of the expected BRAF(V600E)-harboring cell lines consistent with its kinome selectivity profile. These results suggest that rigidification could be a general and powerful strategy for enhancing inhibitor selectivity against protein kinases, which may open up therapeutic opportunities not afforded by other approaches.

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Assadieskandar, A; Yu, CQ; Maisonneuve, P; Kunnov, I; Sicheri, F; Zhang, C or concate me.. Quality Control of 3-(Trifluoromethyl)phenol

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

Category: indole-building-block. In 2020.0 J ORGANOMET CHEM published article about IN-SITU PYROLYSIS; SELECTIVE OXIDATION; BENZYL ALCOHOL; CO2 CAPTURE; MOFS; SEPARATION; ADSORPTION; ALDEHYDES; CAPACITY in [Sabaghi, Maryam; Aghajani, Zahra; Najafi, Gholam Reza] Islamic Azad Univ, Dept Chem, Qom Branch, Qom, Iran in 2020.0, Cited 46.0. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6.

Ultrasonic-assisted reactions, as a green technique, are often more efficient compared to those traditional protocols. To this end, the selective and solvent-free oxidation of aromatic alcohols to the corresponding aldehydes and ketones were investigated in the presence of Co-ABDC/W at room temperature under ultrasonic irradiation conditions for the first time in this paper. The structure, particle size, thermal stability, and morphology of the fabricated heterogeneous catalyst and the products were characterized by FT-IR, EDS, FE-SEM, XRD, TGA, and GC analyses. In this regard, immobilization of tungstate had a significant effect on thermal stability (around 450 degrees C for 40% weight loss) and catalytic performance. Moreover, the efficiency of two different oxidation methods, including ultrasound irradiations and reflux, were comparatively investigated by GC spectrometry. Obtained sonoxidation results presented higher conversions ranging (84 to 100%) than reflux condition via shorter reaction times. The influences of the reaction parameters, such as hydrogen peroxide concentration, and catalyst loading, were also investigated. The proposed method offers several advantages, such as excellent conversions, selective oxidations, environmentally-benign procedure, short reaction times, and easy workup. Notably, this is the first report that focuses on using amino-functionalized MOFs with ultrasonic irradiation for selective oxidation reactions. (C) 2020 Elsevier B.V. All rights reserved.

Category: indole-building-block. About Benzyl Alcohol, If you have any questions, you can contact Sabaghi, M; Aghajani, Z; Najafi, GR 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

Product Details of 150-76-5. Authors Ghosh, P; Maity, T; Biswas, S; Debnath, R; Koner, S in PERGAMON-ELSEVIER SCIENCE LTD published article about in [Ghosh, Pameli; Maity, Tanmoy; Debnath, Rakesh; Koner, Subratanath] Jadavpur Univ, Dept Chem, Kolkata 700032, India; [Maity, Tanmoy] Indian Inst Sci, Solid State & Struct Chem Unit, Bangalore 560012, Karnataka, India; [Biswas, Saptarshi] Katwa Coll, Katwa 713130, W Bengal, India in 2021, Cited 120. The Name is Mequinol. Through research, I have a further understanding and discovery of 150-76-5

Hydrothermal treatment of gadolinium nitrate and 2,6-naphthalenedicarboxylic acid (H2NDC) afforded a new metal-organic framework compound, {[Gd-4(NDC)(6)(H2O)(6)]center dot 2H(2)O}n(1). Compound 1 has been characterized by single-crystal X-ray crystallography, elemental analysis, FT-IR spectroscopy, therrmogravimetric analysis (TGA) and powder X-ray diffraction analysis. It is crystallized in the monoclinic system with the P2(1)/n space group. Four crystallographically distinct Gd (III) centres are interconnected with each other through bridged carboxylato oxygen atoms and water molecules to form tetranuclear secondary building units, which are further connected through the carboxylato ligand and the network propagates along the crystallographic ac plane to form a 2D structure. Subsequent reinforcement from the remaining carboxylato oxygen atoms gives rise to a robust 3D framework structure. Thermogravimetric analysis demonstrates that compound 1 is fairly stable after dehydration under a nitrogen atmosphere. Notably, compound 1 is capable of catalyzing the O-arylation reaction efficiently between substituted phenols and bromoarene under heterogeneous conditions at 80 degrees C to afford unsymmetrical diarylethers. (C) 2020 Elsevier Ltd. All rights reserved.

Product Details of 150-76-5. About Mequinol, If you have any questions, you can contact Ghosh, P; Maity, T; Biswas, S; Debnath, R; Koner, S 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

Recently I am researching about FACTOR RECEPTOR KINASE; SUBSTITUTED QUINOLINONES; PYRAZOLE DERIVATIVES; POTENTIAL ANTICANCER; ERLOTINIB; CANCER; CRIZOTINIB; CHEMISTRY; ASSAY, Saw an article supported by the . Published in ACADEMIC PRESS INC ELSEVIER SCIENCE in SAN DIEGO ,Authors: Elbastawesy, MAI; Aly, AA; Ramadan, M; Elshaier, YAMM; Youssif, BGM; Brown, AB; Abuo-Rahma, GEDA. The CAS is 86-95-3. Through research, I have a further understanding and discovery of 4-Hydroxyquinolin-2(1H)-one. Product Details of 86-95-3

Two new series of diethyl 2-[2-(substituted-2-oxo-1,2-dihydroquinolin-4-yl)hydrazono]-succinates 6a-g and 1-(2-oxo-1,2-dihydroquinolin-4-yl)-1H-pyrazoles 7a-f have been designed and synthesized. The structures of the synthesized compounds were proved by IR, mass, NMR (2D) spectra and elemental analyses. The target compounds were evaluated for their in vitro cytotoxic activity against 60 cancer cell lines according to NCI protocol. Consequently, seven compounds were further examined against the most sensitive cell lines, leukemia CCRFCEM, and MOLT-4. 5-Amino-1-(6-bromo-2-oxo-1,2-dihydroquinolin-4-yl)-1H-pyrazole-3,4-dicarbonitrile (7f) was the most active product, with IC50= 1.35 uM and 2.42 uM against MOLT-4 and CCRF-CEM, respectively. Also, it showed a remarkable inhibitory activity compared to erlotinib on the EGFR TK with IC50 = 247.14 nM and 208.42 nM, respectively. Cell cycle analysis of MOLT-4 cells treated with 7f showed cell cycle arrest at G2/M phase (supported by Caspases, BAX and Bcl-2 studies) with a significant pro-apoptotic activity as indicated by annexin V-FITC staining. Moreover, the docking study indicated that both the pyrazole moiety and the quinolin-2-one ring showed good fitting into EGFR (PDB code: 1M17). In order to interpret SAR of the designed compounds, and provide a basis for further optimization, molecular docking of the synthesized compounds to known EGFR inhibitors was performed. The study illustrated the effect of several factors on the compounds’ activity.

Product Details of 86-95-3. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Elbastawesy, MAI; Aly, AA; Ramadan, M; Elshaier, YAMM; Youssif, BGM; Brown, AB; Abuo-Rahma, GEDA 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

I found the field of Pharmacology & Pharmacy; Virology very interesting. Saw the article Host RNA quality control as a hepatitis B antiviral target published in 2021. Computed Properties of C9H7NO2, Reprint Addresses Block, TM (corresponding author), Baruch S Blumberg Inst, Doylestown, PA 18902 USA.. The CAS is 86-95-3. Through research, I have a further understanding and discovery of 4-Hydroxyquinolin-2(1H)-one

Inhibition of the host RNA polyadenylating polymerases, PAPD5 and PAPD7 (PAPD5/7), with dihydroquinolizinone, a small orally available, molecule, results in a rapid and selective degradation of hepatitis B virus (HBV) RNA, and hence reduction in the amounts of viral gene products. DHQ, is a first in class investigational agent and could represent an entirely new category of HBV antivirals. PAPD5 and PAPD7 are noncanonical, cell specified, polyadenylating polymerases, also called terminal nucleotidyl transferases 4B and 4A (TENT4B/A), respectively. They are involved in the degradation of poor-quality cell transcripts, mostly noncoding RNAs and in the maturation of a sub-set of transcripts. They also appear to play a role in shielding some mRNA from degradation. The results of studies with DHQ, along with other recent findings, provide evidence that repression of the PAPD5/7 arm of the cell RNA quality control pathway, causes a profound (multifold) reduction rather than increase, in the amount of HBV pre-genomic, pre-core and HBsAg mRNA levels in tissue culture and animal models, as well. In this review we will briefly discuss the need for new HBV therapeutics and provide background about HBV transcription. We also discuss cellular degradation of host transcripts, as it relates to a new family of anti-HBV drugs that interfere with these processes. Finally, since HBV mRNA maturation appears to be selectively sensitive to PAPD5/7 inhibition in hepatocytes, we discuss the possibility of targeting host RNA quality control as an antiviral strategy.

About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Block, TM; Young, JAT; Javanbakht, H; Sofia, MJ; Zhou, TL or concate me.. Computed Properties of C9H7NO2

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

COA of Formula: C9H7NO2. Authors Aly, AA; Hassan, AA; Mohamed, NK; Abd El-Haleem, LE; Brase, S in SAGE PUBLICATIONS LTD published article about in [Aly, Ashraf A.; Hassan, Alaa A.; Mohamed, Nasr K.; Abd El-Haleem, Lamiaa E.] Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt; [Brase, Stefan] Karlsruhe Inst Technol, Inst Biol & Chem Syst Funct Mol Syst IBCS FMS, Eggenstein Leopoldshafen, Germany in 2020, Cited 13. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3

A novel series of 7,8-dichlorobenzofuro[3,2-c]quinoline-6,9,10(5H)-triones was obtained regioselectively in good yields. The products were formed by the reactions of the 4-hydroxy-2(1H)-quinolinones with 3,4,5,6-tetrachloro-1,2-benzoquinone in tetrahydrofuran as the solvent. Infrared, nuclear magnetic resonance (two-dimensional nuclear magnetic resonance), mass spectra and elemental analysis were used to elucidate the structures of new compounds.

COA of Formula: C9H7NO2. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Aly, AA; Hassan, AA; Mohamed, NK; Abd El-Haleem, LE; Brase, S 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

Authors Sun, YY; Gao, PP; Zhu, L; Li, ZX; Zhao, RY; Li, CY; Shan, LH in ELSEVIER SCIENCE INC published article about ABIRATERONE ACETATE; NECROPTOSIS; PYRIDINES; INHIBITOR; CHEMISTRY; DESIGN in [Sun, Yingying; Gao, Peipei; Li, Zhaoxiang; Zhao, Ruiyun; Shan, Lihong] Zhengzhou Univ, Sch Pharmaceut Sci, Key Lab Adv Drug Preparat Technol, Minist Educ, Zhengzhou 450001, Peoples R China; [Sun, Yingying; Gao, Peipei; Li, Zhaoxiang; Zhao, Ruiyun; Shan, Lihong] Collaborat Innovat Ctr New Drug Res & Safety Eval, Zhengzhou, Henan, Peoples R China; [Zhu, Li] Shanxi Med Univ, Taiyuan Cent Hosp, 5 Dong San Dao Xiang, Taiyuan 030009, Peoples R China; [Li, Congyu] Zhengzhou Univ, Henan Canc Hosp, Affiliated Canc Hosp, Zhengzhou, Peoples R China in 2021.0, Cited 34.0. Recommanded Product: 123-11-5. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5

A series of new 17-cyanopyridine derivatives of pregnenolone have been synthesized, and their anti-proliferative activities against different human cancer cell lines were tested. The extensive structure-activity relationship (SAR) data suggested that the introduction of 2-amino-4-aryl-3-cyanopyridine to the D ring of pregnenolone may increase the anti-cancer activity. Among the products, the most potent compound 4j exhibited good growth inhibition against all the tested cells especially for PC- 3 cells with an IC50 value of 2.0 mu M. Further mechanistic studies showed that 4j inhibited the formation of cell colonies and migration, increased the level of reactive oxygen species (ROS) in PC-3 cells in a concentration-dependent manner, and induced necroptosis through the phosphorylation of receptor interacting protein 1/3 (P-RIP1/3) and phosphorylation of mixed lineage kinase domain-like protein (P-MLKL) pathway. The 17-pregnenolone cyanopyridine derivatives hold promising potential as anti-proliferative agents, and the most potent compound could be used as a starting point for the development of new steroidal heterocycles with improved anticancer potency and selectivity.

About 4-Methoxybenzaldehyde, If you have any questions, you can contact Sun, YY; Gao, PP; Zhu, L; Li, ZX; Zhao, RY; Li, CY; Shan, LH or concate me.. Recommanded Product: 123-11-5

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 Chemistry very interesting. Saw the article Sulfonated-polyvinyl amine coated on Fe3O4 nanoparticles: a high-loaded and magnetically separable acid catalyst for multicomponent reactions published in 2019.0. COA of Formula: C7H6O2, Reprint Addresses Koukabi, N (corresponding author), Semnan Univ, Dept Chem, POB 35195-363, Semnan, Iran.. The CAS is 100-83-4. Through research, I have a further understanding and discovery of 3-Hydroxybenzaldehyde

In this study, a PVAm-bearing SO3H groups/Fe3O4 nanocomposite was prepared via a simple and in situ polymerization of acrylamide onto the surface of magnetic nanoparticles without using organosilane precursors. In order to obtain amine-functionalized magnetic, Hofmann degradation was carried out. In the following, sulfonated-polyvinyl amine coated on Fe3O4 nanoparticles was prepared by covalent grafting of chlorosulfonic acid on amine groups. The introduction of polymer to the surface of magnetic nanoparticles increases the loading content with functional groups extremely. The resulting hybrid material was effectively employed as an unprecedented acid magnetic catalyst for the one-pot synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazoles under solvent-free conditions. High yields, mild reaction conditions, short reaction times, operational simplicity with reusability are the notable features of the catalyst. The structure of the newly developed catalyst was characterized using TGA, FT-IR, SEM, TEM, VSM, EDX, CHNS, and XRD analysis. Magnetic separation and recycling of the catalyst for at least 8 runs is possible without any significant deterioration in catalytic activity. This work is the first report of employing PVAm as a linker for immobilizing liquid acid on a support.

COA of Formula: C7H6O2. About 3-Hydroxybenzaldehyde, If you have any questions, you can contact Arghan, M; Koukabi, N; Kolvari, E 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

Ma, C; Zhao, CQ; Xu, XT; Li, ZM; Wang, XY; Zhang, K; Mei, TS in [Ma, Cong; Zhao, Chuan-Qi; Li, Zhao-Ming; Mei, Tian-Sheng] Chinese Acad Sci, Shanghai Inst Organ Chem, Ctr Excellence Mol Synth, State Key Lab Organometall Chem, 345 Lingling Lu, Shanghai 200032, Peoples R China; [Xu, Xue-Tao; Wang, Xiang-Yang; Zhang, Kun] Wuyi Univ, Sch Chem & Environm Engn, Jiangmen 529020, Peoples R China published Nickel-Catalyzed Carboxylation of Aryl and Heteroaryl Fluorosulfates Using Carbon Dioxide in 2019, Cited 67. Name: 4′-Hydroxyacetophenone. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4.

The development of efficient and practical methods to construct carboxylic acids using CO2 as a C1 synthon is of great importance. Nickel-catalyzed carboxylation of aryl fluorosulfates and heteroaryl fluorosulfates with CO2 is described, affording arene carboxylic acids with good to excellent yields under mild conditions. In addition, a one-pot phenol fluorosulfation/carboxylation is developed.

Name: 4′-Hydroxyacetophenone. About 4′-Hydroxyacetophenone, If you have any questions, you can contact Ma, C; Zhao, CQ; Xu, XT; Li, ZM; Wang, XY; Zhang, K; Mei, TS 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

Application In Synthesis of Benzyl Alcohol. Recently I am researching about ACID PHENETHYL ESTER; REPERFUSION INJURY; PROPOLIS; HYPERURICEMIA; INTEGRASE; DISCOVERY, Saw an article supported by the National Institutes of HealthUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USA [5P20GM103436, 2R15GM084431-02A1]; NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCESUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USANIH National Institute of General Medical Sciences (NIGMS) [P20GM103436] Funding Source: NIH RePORTER. Published in ACADEMIC PRESS INC ELSEVIER SCIENCE in SAN DIEGO ,Authors: Choi, W; Villegas, V; Istre, H; Heppler, B; Gonzalez, N; Brusman, N; Snider, L; Hogle, E; Tucker, J; Onate, A; Onate, S; Ma, LL; Paula, S. The CAS is 100-51-6. Through research, I have a further understanding and discovery of Benzyl Alcohol

Inhibitors of the enzyme xanthine oxidase (XO) with radical scavenging properties hold promise as novel agents against reperfusion injuries after ischemic events. By suppressing the formation of damaging reactive oxygen species (ROS) by XO or scavenging ROS from other sources, these compounds may prevent a buildup of ROS in the aftermath of a heart attack or stroke. To combine these two properties in a single molecule, we synthesized and characterized the non-purine XO inhibitor caffeic acid phenethylester (CAPE) and 19 derivatives using a convenient microwave-assisted Knoevenagel condensation protocol. Varying systematically the number and positions of the hydroxyl groups at the two phenyl rings, we derived structure-activity relationships based on experimentally determined XO inhibition data. Molecular docking suggested that critical enzyme/inhibitor interactions involved pi-pi interactions between the phenolic inhibitor ring and Tyr914, hydrogen bonds between inhibitor hydroxyl groups and Glu802, and hydrophobic interactions between the CAPE phenyl ring and nonpolar residues located at the entrance of the binding site. To effectively scavenge the stable radical DPPH, two hydroxyl groups in 1,2-or 1,4-position at the phenyl ring were required. Among all compounds tested, E-phenyl 3-(3,4-dihydroxyphenyl)acrylate, a CAPE analog without the ethyl tether, showed the most promising properties.

Application In Synthesis of Benzyl Alcohol. About Benzyl Alcohol, If you have any questions, you can contact Choi, W; Villegas, V; Istre, H; Heppler, B; Gonzalez, N; Brusman, N; Snider, L; Hogle, E; Tucker, J; Onate, A; Onate, S; Ma, LL; Paula, S 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