Day: January 14, 2022

Authors Choo, HJ; Ahn, JH in AMER CHEMICAL SOC published article about MICROBIAL-PRODUCTION; SALICYLATE BIOSYNTHESIS; PURIFICATION; ENZYME in [Choo, Hye Jeong; Ahn, Joong-Hoon] Konkuk Univ, Bio Mol Informat Ctr, Dept Biosci & Biotechnol, Seoul 05029, South Korea in 2019, Cited 31. Formula: C9H7NO2. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3

Intermediates in aromatic amino acid biosynthesis can serve as substrates for the synthesis of bioactive compounds. In this study we used two intermediates in the shikimate pathway of Escherichia coli, chorismate and anthranilate, to synthesize three bioactive compounds: 4-hydroxycoumarin (4-HC), 2,4-dihydroxyquinoline (DHQ), and 4-hydroxy-1-methyl-2(1H)-quinolone (NMQ). We introduced genes for the synthesis of salicylic acid from chorismate to supply the substrate for 4-HC and the gene encoding N-methyltransferase for the synthesis of N-methylanthranilate from anthranilate. Polyketide synthases and coenzyme (Co)A ligases were tested to determine the optimal combination of genes for the synthesis of each compound. We also tested several constructs and identified the best one for increasing levels of endogenous substrates for chorismate, anthranilate, and malonyl-CoA. With the use of these strategies, 255.4 mg/L 4-HC, 753.7 mg/L DHQ, and 17.5 mg/L NMQwere synthesized. This work provides a basis for the synthesis of diverse coumarin and quinoline derivatives with potential medical applications.

SDS of cas: 86-95-3. Bye, fridends, I hope you can learn more about C9H7NO2, 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

An article Discovery of 4H-Chromen-4-one Derivatives as a New Class of Selective Rho Kinase (ROCK) Inhibitors, which Showed Potent Activity in ex Vivo Diabetic Retinopathy Models WOS:000503114200013 published article about RETINAL EXPLANT CULTURES; PHOSPHORYLATION in [Zhao, Lanying; Li, Yueshan; Qiao, Zeen; Miao, Zhuang; Yang, Jiao; Huang, Luyi; Yang, Shengyong] Sichuan Univ, West China Hosp, State Key Lab Biotherapy, Chengdu 610041, Sichuan, Peoples R China; [Zhao, Lanying; Li, Yueshan; Qiao, Zeen; Miao, Zhuang; Yang, Jiao; Huang, Luyi; Yang, Shengyong] Sichuan Univ, West China Hosp, Canc Ctr, Chengdu 610041, Sichuan, Peoples R China; [Wang, Yujiao; Chen, Danian] Sichuan Univ, West China Hosp, Dept Ophthalmol, Research Lab Ophthalmol & Vis Sci, Chengdu 610041, Sichuan, Peoples R China; [Tian, Chenyu; Li, Linli] Sichuan Univ, West China Sch Pharm, Key Lab Drug Targeting & Drug Delivery Syst, Minist Educ, Chengdu 610041, Sichuan, Peoples R China in 2019.0, Cited 27.0. The Name is m-Methoxyphenol. Through research, I have a further understanding and discovery of 150-19-6. Application In Synthesis of m-Methoxyphenol

Diabetic retinopathy (DR) is a major cause of blindness, and there is a lack of effective treatment at present. Rho-associated coiled-coil containing serine/threonine protein kinases (ROCKs) have recently been suggested as potential targets for the DR treatment. We herein report the discovery of 4H-chromen-4-one derivatives as a new class of ROCK inhibitors. Structure-activity relationship analyses led to the identification of the most active compound, 4-(dimethylamino)-N-(3-{2-[(4-oxo-4H-chromen-7-yl)oxy]acetamido}phenyl) (12j). This compound showed excellent kinase selectivity for ROCK I and ROCK II against 387 other kinases. In retinal explants, compound 12j protected retinal neurons from high glucose-induced oxidative stress and apoptosis-mediated cell death. Furthermore, 12j administration suppressed the improper proliferation of Muller cells and promoted the regression of vascular vessels in retinal explants cultured in a high glucose microenvironment. Collectively, our data suggest that 12j could be a potential lead compound for the treatment of DR, hence deserving further in-depth studies.

Application In Synthesis of m-Methoxyphenol. Welcome to talk about 150-19-6, If you have any questions, you can contact Zhao, LY; Li, YS; Wang, YJ; Qiao, Z; Miao, Z; Yang, J; Huang, LY; Tian, CY; Li, LL; Chen, DN; Yang, SY 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 Synthesis and in vitro antimycobacterial potential of novel hydrazones of eugenol WOS:000514837800079 published article about ANTIBACTERIAL ACTIVITY; SCHIFF-BASES; DERIVATIVES in [Rohane, Sachin H.] Kadi Sarva Vishwavidyalaya, Dept Pharmaceut Chem, Gandhinagar 382015, India; [Chauhan, Ashlesha J.] KB Inst Pharmaceut Educ & Res, Dept Chem, Gandhinagar 382023, Gujarat, India; [Fuloria, Neeraj Kumar; Fuloria, Shivkanya] AIMST Univ, Fac Pharm, Bedong 08100, Kedah, Malaysia in 2020.0, Cited 17.0. Product Details of 99-93-4. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4

Fifty one hydrazone derivatives of eugenol were designed and docked with 2NSD and 2X22 (enzymes of H37Rv strain) using Schrodinger v7.4. The selective ten hydrazone derivatives (4, 5, 11, 18, 30, 34, 35, 37, 42, and 45) of eugenol were synthesized via esterification, hydrazination and treatment with different aldehydes. Synthesized compounds were characterized by IR, H-1 NMR, and LCMS data. The compounds were evaluated for their antitubercular potential against H37Rv using microplate alamar blue assay (MABA). The study revealed that all synthesized compounds were significantly active at concentration 50 and 100 mu g/ml, whereas compound 11 exhibited activity at 25 mu g/ml. Present study showed that antitubercular activity of novel hydrazone derivatives of eugenol is strongly connected with the position of the substituent on aromatic aldehyde or ketones. (C) 2019 Production and hosting by Elsevier B.V. on behalf of King Saud University.

Product Details of 99-93-4. 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.

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 Sundar, MS; Klepetarova, B; Bednarova, L; Muller, G in WILEY-V C H VERLAG GMBH published article about ONE HUNDRED YEARS; STEREOSELECTIVE SYNTHESES; ENANTIOMERICALLY PURE; STRUCTURAL-PROPERTIES; HELICAL QUINONE; OXAHELICENES; ROUTE in [Sundar, M. Shyam; Klepetarova, Blanka; Bednarova, Lucie] Czech Acad Sci, Inst Organ Chem & Biochem, Flemingovo Namesti 2, Prague 16610, Czech Republic; [Muller, Gilles] San Jose State Univ, Dept Chem, One Washington Sq, San Jose, CA 95192 USA in 2021.0, Cited 56.0. Recommanded Product: 150-76-5. The Name is Mequinol. Through research, I have a further understanding and discovery of 150-76-5

Herein, we report a simple and efficient approach to synthesize a functionalized 2,18-dimethoxy-5,10,15-trioxa[9]helicene. It was synthesized from simple phenol building blocks using two subsequent reactions namely oxidative coupling and dehydrative cyclization or palladium mediated cyclization. The molecular integrity of the helical core was determined by single-crystal X-ray diffraction and NMR techniques. Its crystal structure showed the spontaneous resolution which was attributed to the conglomerate formation of the same helical isomer via C-H…O and pi…pi or H…pi interactions. Then, it was converted to racemic 2,18-dihydoxy-5,10,15-trioxa[9]helicene. Enantiomers were separated on preparative HPLC with high optical purity (>99 % ee). Based on electronic circular dichroism, the absolute configurations of dextrorotary and levorotatory antipodes were assigned as P and M, respectively. We also studied the absorption, emission and chiroptical behavior of these helical compounds in the solution state.

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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

SDS of cas: 86-95-3. 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.

SDS of cas: 86-95-3. Welcome to talk about 86-95-3, If you have any questions, you can contact Aly, AA; Hassan, AA; Mohamed, NK; Abd El-Haleem, LE; Brase, S 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

Product Details of 86-95-3. Aly, AA; El-Sheref, EM; Bakheet, MEM; Mourad, MAE; Brase, S; Ibrahim, MAA; Nieger, M; Garvalov, BK; Dalby, KN; Kaoud, TS in [Aly, Ashraf A.; El-Sheref, Essmat M.; Bakheet, Momtaz E. M.; Ibrahim, Mahmoud A. A.] Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt; [Mourad, Mai A. E.] Port Said Univ, Med Chem Dept, Fac Pharm, Port Said 42526, Egypt; [Kaoud, Tamer S.] Menia Univ, Fac Pharm, Dept Med Chem, El Minia 61519, Egypt; [Brase, Stefan] Karlsruhe Inst Technol, Inst Toxikol & Genet, Hermann von Helmholts Pl 1,Campus Nord, D-76344 Eggenstein Leopoldsha, Germany; [Brase, Stefan] Inst Toxikol & Genet, Hermann von Helmholts Pl 1,Campus Nord, D-76344 Eggenstein Leopoldsha, Germany; [Nieger, Martin] Univ Helsinki, Dept Chem, POB 55, Helsinki 00014, Finland; [Garvalov, Boyan K.] Mannhe Univ Heidelberg, Ctr Biomed & Med Technol Mannheim, Med Fac, D-68167 Mannheim, Germany; [Dalby, Kevin N.; Kaoud, Tamer S.] Univ Texas Austin, Div Chem Biol & Med Chem, Austin, TX 78712 USA published Design, synthesis and biological evaluation of fused naphthofuro[3,2-c]quinoline-6,7,12-triones and pyrano[3,2-c]quinoline-6,7,8,13-tetraones derivatives as ERK inhibitors with efficacy in BRAF-mutant melanoma in 2019, Cited 57. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3.

Approximately 60% of human cancers exhibit enhanced activity of ERK1 and ERK2, reflecting their multiple roles in tumor initiation and progression. Acquired drug resistance, especially mechanisms associated with the reactivation of the MAPK (RAF/MEK/ERK) pathway represent a major challenge to current treatments of melanoma and several other cancers. Recently, targeting ERK has evolved as a potentially attractive strategy to overcome this resistance. Herein, we report the design and synthesis of novel series of fused naphthofuro[3,2-c] quinoline-6,7,12-triones 3a-f and pyrano[3,2-c]quinoline-6,7,8,13-tetraones 5a,b and 6, as potential ERK inhibitors. New inhibitors were synthesized and identified by different spectroscopic techniques and X-ray crystallography. They were evaluated for their ability to inhibit ERK1/2 in an in vitro radioactive kinase assay. 3b and 6 inhibited ERK1 with IC50s of 0.5 and 0.19 mu M, and inhibited ERK2 with IC50s of 0.6 and 0.16 mu M respectively. Kinetic mechanism studies revealed that the inhibitors are ATP-competitive inhibitors where 6 inhibited ERK2 with a K-i of 0.09 mu M. Six of the new inhibitors were tested for their in vitro anticancer activity against the NCI-60 panel of tumor cell lines. Compound 3b and 6 were the most potent against most of the human tumor cell lines tested. Moreover, 3b and 6 inhibited the proliferation of the BRAF mutant A375 melanoma cells with IC50s of 3.7 and 0.13 mu M, respectively. In addition, they suppressed anchorage-dependent colony formation. Treatment of the A375 cell line with 3b and 6 inhibited the phosphorylation of ERK substrates p-90RSK and ELK-1 and induced apoptosis in a dose dependent manner. Finally, a molecular docking study showed the potential binding mode of 3b and 6 within the ATP catalytic binding site of ERK2.

Product Details of 86-95-3. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Aly, AA; El-Sheref, EM; Bakheet, MEM; Mourad, MAE; Brase, S; Ibrahim, MAA; Nieger, M; Garvalov, BK; Dalby, KN; Kaoud, 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

SDS of cas: 86-95-3. In 2020 MONATSH CHEM published article about DERIVATIVES; INHIBITORS; FUROQUINOLINE; ALKALOIDS; MODEL in [Aly, Ashraf A.; Mohamed, Asmaa H.] Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt; [Ishak, Esam] Al Azhar Univ, Fac Sci, Dept Chem, Assiut, Egypt; [Ishak, Esam] Jouf Univ, Coll Sci & Arts, Dept Chem, Alquurrayate, Saudi Arabia; [Shwaky, Ahmed M.] Umm Al Qura Univ, STU, Mecca, Saudi Arabia in 2020, Cited 31. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3.

Quinoline-2,4-diones reacted with 2-[bis(methylthio)methylene]malononitrile in DMF/Et3N to produce 3-(methylthio)-4-oxo-4,5-dihydrofuro[3,2-c]quinolone-2-carbonitriles and 3-(methylthio)-4-oxo-4,5-dihydrofuro[3,2-c]quinolone-2-carboxamides in state of 2-imino-substituted 4-(methylthio)-5,6-dihydro-2H-pyrano[3,2-c]quinolone-3-carbonitriles. The structures of all new products were proved using NMR, IR, and mass spectral data. The possible mechanism for the reaction is also discussed. Graphic abstract

SDS of cas: 86-95-3. Welcome to talk about 86-95-3, If you have any questions, you can contact Aly, AA; Ishak, E; Shwaky, AM; Mohamed, AH 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

Authors Li, YX; Li, XQ; Li, XW; Shi, DY in ROYAL SOC CHEMISTRY published article about in [Li, Yuxiu; Li, Xiangqian; Li, Xiaowei; Shi, Dayong] Shandong Univ, State Key Lab Microbial Technol, 72 Binhai Rd, Qingdao 266237, Shandong, Peoples R China; [Li, Yuxiu; Li, Xiangqian; Li, Xiaowei; Shi, Dayong] Shandong Univ, Marine Biotechnol Res Ctr, 72 Binhai Rd, Qingdao 266237, Shandong, Peoples R China; [Shi, Dayong] Pilot Natl Lab Marine Sci & Technol, Lab Marine Biol & Biotechnol, 168 Wenhai Rd, Qingdao 266237, Shandong, Peoples R China in 2021.0, Cited 60.0. Application In Synthesis of 3,4-Dimethoxybenzaldehyde. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

Regioselective synthesis of alpha-fluoro-beta-arylalkenyl sulfides has been established with gem-difluoroalkenes and sodium sulfinates in a transition-metal-free manner. A series of control experiments were executed to demonstrate thiol radicals and anions as the proposed intermediates. Notably, regioselective Z -> E isomerization was achieved under green light irradiation in the absence of a photoinitiator.

Bye, fridends, I hope you can learn more about C9H10O3, If you have any questions, you can browse other blog as well. See you lster.. COA of Formula: C9H10O3

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 4′-Hydroxyacetophenone. Recently I am researching about DERIVATIVES; CHALCONE; DESIGN; AMONAFIDE; DOCKING; INHIBITORS; APOPTOSIS; BINDING; BCL-2, Saw an article supported by the Department of Science and Technology (DST), New Delhi, India, under INSPIRE programmeDepartment of Science & Technology (India)Department of Science & Technology (DOST), Philippines [Shalini IF160180]; National Research Foundation South AfricaNational Research Foundation – South Africa [121276]. Published in ROYAL SOC CHEMISTRY in CAMBRIDGE ,Authors: Shalini; Pankaj; Saha, ST; Kaur, M; Oluwakemi, E; Awolade, P; Singh, P; Kumar, V. The CAS is 99-93-4. Through research, I have a further understanding and discovery of 4′-Hydroxyacetophenone

A series of naphthalimide-chalcone/pyrazoline conjugates was prepared and evaluated for their anti-breast cancer potential against estrogen responsive, i.e. MCF-7 (ER+), and triple-negative, i.e. MDA-MB-231 (ER-), cell lines. The structure-activity-relationship (SAR) was deduced based on the influence of linker length, substituents on the phenyl ring and the generated functionalities, on anti-proliferative activities. Docking simulations further delineate the type of interactions of the designed molecules with the selected targets. This report discloses the scope of triazole tethered naphthalimide-chalcone/pyrazoline conjugates as anti breast cancer agents.

Welcome to talk about 99-93-4, If you have any questions, you can contact Shalini; Pankaj; Saha, ST; Kaur, M; Oluwakemi, E; Awolade, P; Singh, P; Kumar, V or send Email.. Application In Synthesis of 4′-Hydroxyacetophenone

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: C8H8O2. In 2019.0 TETRAHEDRON LETT published article about ELECTRON-SPIN-RESONANCE; C-H FUNCTIONALIZATION; DERIVATIVES; BIOACTIVITY; OXIDATION; KETOXIMES; ANALOGS; DESIGN; AGENTS in [Han, Ziwei; Shen, Subo; Hu, Han; Zhang, Jianmin] Shanghai Univ, Coll Sci, Dept Chem, Shanghai 200444, Peoples R China; [Zheng, Feng] Shanghai Aerosp Chem Applicat Res Inst, Shanghai 201109, Peoples R China; [Zhang, Jianmin; Zhu, Shizheng] Chinese Acad Sci, Shanghai Inst Organ Chem, Key Lab Organofluorine Chem, 345 Lingling Rd, Shanghai 200032, Peoples R China in 2019.0, Cited 40.0. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4.

An efficient Cu(II)-catalyzed radical addition of maleimides has been achieved. The identified copper catalyst enables the formation of oxime radicals (N-O-center dot) by cleaving the O-H bond in ketoximes, followed by the radical addition to N-substituted maleimides. The oxime radicals (N-O-center dot) were detected and confirmed by EPR spectroscopy and variable-temperature H-1 NMR. The simple one-pot reaction realizes the facile preparation of a variety of oxime ether adduct products in moderate to good yields. (C) 2019 Elsevier Ltd. All rights reserved.

COA of Formula: C8H8O2. 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.

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