Interesting scientific research on 4-Hydroxyquinolin-2(1H)-one

Quality Control of 4-Hydroxyquinolin-2(1H)-one. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Marjani, AP; Khalafy, J; Farajollahi, A or concate me.

Quality Control of 4-Hydroxyquinolin-2(1H)-one. In 2019 J HETEROCYCLIC CHEM published article about TETRAPROPYLAMMONIUM BROMIDE; BIOLOGICAL EVALUATION; DERIVATIVES; CATALYST; WATER in [Marjani, Ahmad Poursattar; Khalafy, Jabbar; Farajollahi, Ayda] Urmia Univ, Dept Organ Chem, Fac Chem, Orumiyeh, Iran in 2019, Cited 41. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3.

In this research, in order to synthesize a series of ethyl 2-amino-4-benzoyl-5-oxo-5,6-dihydro-4H-pyrano[3,2-c]quinoline-3-carboxylates, a green and an efficient method is proposed through one-pot three-component reaction of substituted arylglyoxals, ethyl cyanoacetate, and 4-hydroxyquinolin-2(1H)-one in the presence of terapropylammonium bromide as a catalyst in good yields. All synthesized new substances were characterized by FTIR, H-1-NMR, and C-13-NMR spectral data and elemental analysis.

Quality Control of 4-Hydroxyquinolin-2(1H)-one. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Marjani, AP; Khalafy, J; Farajollahi, A 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

Can You Really Do Chemisty Experiments About C9H7NO2

Computed Properties of 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; Polamo, M; Nieger, M; Brown, AB or concate me.

Aly, AA; Hassan, AA; Mohamed, NK; Abd El-Haleem, LE; Brase, S; Polamo, M; Nieger, M; Brown, AB 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; [Braese, Stefan] Karlsruhe Inst Technol, Inst Organ Chem, D-76131 Karlsruhe, Germany; [Braese, Stefan] Karlsruhe Inst Technol, Inst Toxicol & Genet, D-76344 Eggenstein Leopoldshafen, Germany; [Polamo, Mika; Nieger, Martin] Univ Helsinki, Dept Chem, POB 55,AI Virtasen Aukio 1, Helsinki 00014, Finland; [Brown, Alan B.] Florida Inst Technol, Chem Program, Melbourne, FL 32901 USA published Synthesis of New Fused Heterocyclic 2-Quinolones and 3-Alkanonyl-4-Hydroxy-2-Quinolones in 2019, Cited 31. Computed Properties of C9H7NO2. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3.

Herein, we report the synthesis of 5,12-dihydropyrazino[2,3-c:5,6-c ‘]difuro[2,3-c:4,5-c ‘]-diquinoline-6,14(5H,12H)diones, 2-(4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)-1,4-diphenyl- butane-1,4-diones and 4-(benzo-[d]oxazol-2-yl)-3-hydroxy-1H-[4,5]oxazolo[3,2-a]pyridine-1-one. The new candidates were synthesized and identified by different spectroscopic techniques, and X-ray crystallography.

Computed Properties of 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; Polamo, M; Nieger, M; Brown, AB 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

Final Thoughts on Chemistry for 3,4-Dimethoxybenzaldehyde

About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Zhang, S; Li, LJ; Li, JJ; Shi, JX; Xu, K; Gao, WC; Zong, LY; Li, GG; Findlater, M or concate me.. Category: indole-building-block

Recently I am researching about C-H FUNCTIONALIZATION; PHOTOREDOX CATALYSIS; CARBONYL-COMPOUNDS; COUPLING REACTIONS; NICKEL CATALYSIS; GRIGNARD; HYDROGEN; HALIDES; IMINES; REAGENTS, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21702113, 22071102, 91956110]; Thousand Talents Plan of Central Plains; Key Scientific Research Projects of Higher Education Institutions in Henan Province [20A150029]; National Science FoundationNational Science Foundation (NSF) [CHE-1554906]; Robert A. Welch FoundationThe Welch Foundation [D-1361]. Published in WILEY-V C H VERLAG GMBH in WEINHEIM ,Authors: Zhang, S; Li, LJ; Li, JJ; Shi, JX; Xu, K; Gao, WC; Zong, LY; Li, GG; Findlater, M. The CAS is 120-14-9. Through research, I have a further understanding and discovery of 3,4-Dimethoxybenzaldehyde. Category: indole-building-block

Arylation of carbonyls, one of the most common approaches toward alcohols, has received tremendous attention, as alcohols are important feedstocks and building blocks in organic synthesis. Despite great progress, there is still a great gap to develop an ideal arylation method featuring mild conditions, good functional group tolerance, and readily available starting materials. We now show that electrochemical arylation can fill the gap. By taking advantage of synthetic electrochemistry, commercially available aldehydes (ketones) and benzylic alcohols can be readily arylated to provide a general and scalable access to structurally diverse alcohols (97 examples, >10 gram-scale). More importantly, convergent paired electrolysis, the ideal but challenging electrochemical technology, was employed to transform low-value alcohols into more useful alcohols. Detailed mechanism study suggests that two plausible pathways are involved in the redox neutral alpha-arylation of benzylic alcohols.

About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Zhang, S; Li, LJ; Li, JJ; Shi, JX; Xu, K; Gao, WC; Zong, LY; Li, GG; Findlater, M or concate me.. Category: indole-building-block

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

Something interesting about C9H10O3

COA of Formula: C9H10O3. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Aziz, MW; Kamal, AM; Mohamed, KO; Elgendy, AA or concate me.

An article Design, synthesis and assessment of new series of quinazolinone derivatives as EGFR inhibitors along with their cytotoxic evaluation against MCF7 and A549 cancer cell lines WOS:000651228800015 published article about GROWTH-FACTOR RECEPTOR; BIOLOGICAL EVALUATION in [Aziz, Marian W.; Elgendy, Adel A.] Misr Int Univ, Fac Pharm, Dept Pharmaceut Chem, Cairo, Egypt; [Kamal, Aliaa M.; Mohamed, Khaled O.] Cairo Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Cairo, Egypt; [Kamal, Aliaa M.] October Univ Modern Sci & Arts MSA, Fac Pharm, Dept Pharmaceut Chem, Giza, Egypt in 2021.0, Cited 43.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9. COA of Formula: C9H10O3

New acetamide (IV a-e) and 1,3-thiazolidinone derivatives (VII a-e) were designed, synthesized and assessed for their cytotoxic activity against MCF-7 and A549 cell lines along with their lead compounds (erlotinib and gefitinib). The newly designed compounds were prepared according to the adopted procedures in schemes 1 and 2 from their quinazolinone parents. 3D QSAR pharmacophore and docking molecular modeling protocols were conducted using Discovery Studio program, beside a full biological assay for these compounds. The cytotoxicity evaluation demonstrated that compounds IVb, IVc, VIIa, VIIb, VIId exhibited potent cytotoxic activities against both MCF-7 and A549 cell lines. Moreover, the molecular modeling studies corroborated to the affinity of the compounds towards EGFR. Consequently, these five compounds were then screened for their EGFR inhibition and evaluated as well for their toxicity to normal cells, which revealed that the acetamide derivative IVc and the thiazolidinone derivative VIIa were the most potent and least toxic. DNA flow cytometry analysis was conducted for compounds IVc and VIIa, which indicated that they both induced arrest at G2/M phase of the cell cycle.

COA of Formula: C9H10O3. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Aziz, MW; Kamal, AM; Mohamed, KO; Elgendy, AA 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

Top Picks: new discover of 3-(Trifluoromethyl)phenol

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Leven, M; Held, J; Duffy, S; Avelar, LAA; Meister, S; Delves, M; Plouffe, D; Kuna, K; Tschan, S; Avery, VM; Winzeler, EA; Mordmuller, B; Kurz, T or concate me.. SDS of cas: 98-17-9

I found the field of Pharmacology & Pharmacy very interesting. Saw the article 8-Aminoquinolines with an Aminoxyalkyl Side Chain Exert in vitro Dual-Stage Antiplasmodial Activity published in 2019. SDS of cas: 98-17-9, Reprint Addresses Kurz, T (corresponding author), Heinrich Heine Univ Dusseldorf, Inst Pharmazeut & Med Chem, Univ Str 1, D-40225 Dusseldorf, Germany.. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol

A series of novel 8-aminoquinolines (8-AQs) with an aminoxyalkyl side chain were synthesized and evaluated for in vitro antiplasmodial properties against asexual blood stages, liver stages, and sexual stages of Plasmodium falciparum. 8-AQs bearing 2-alkoxy and 5-phenoxy substituents on the quinoline ring system were found to be the most promising compounds under study, exhibiting potent blood schizontocidal and moderate tissue schizontocidal in vitro activity.

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Leven, M; Held, J; Duffy, S; Avelar, LAA; Meister, S; Delves, M; Plouffe, D; Kuna, K; Tschan, S; Avery, VM; Winzeler, EA; Mordmuller, B; Kurz, T or concate me.. SDS of cas: 98-17-9

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

Chemical Research in C7H5F3O

Safety of 3-(Trifluoromethyl)phenol. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Zhang, ZP; He, ZQ; Xie, YX; He, TT; Fu, YF; Yu, Y; Huang, F or concate me.

Safety of 3-(Trifluoromethyl)phenol. Authors Zhang, ZP; He, ZQ; Xie, YX; He, TT; Fu, YF; Yu, Y; Huang, F in ROYAL SOC CHEMISTRY published article about in [Zhang, Zhipeng; He, Zhiqin; Xie, Yuxing; Huang, Fei] Nanjing Normal Univ, Sch Food Sci & Pharmaceut Engn, Nanjing 210023, Peoples R China; [Zhang, Zhipeng] South China Univ Technol, Sch Biol & Biol Engn, Guangzhou 510006, Peoples R China; [He, Tiantong; Fu, Yaofeng; Huang, Fei] Nanjing Tech Univ, Sch Pharmaceut Sci, Nanjing 211816, Peoples R China; [Yu, Yang] Nanjing Tech Univ, Sch Environm Sci & Engn, Nanjing 211816, Peoples R China in 2021, Cited 115. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9

Under metal- and ligand-free conditions, the economical and accessible CF3SO3H successfully catalyzed homogeneous O-H bond insertion reactions between hydroxyl compounds and diazo compounds. Including phenols, alcohols, water and oximes, these O-H bond insertion reactions are very general and functional-group tolerant. Here, we first report the O-H bond insertion of oximes (ketoximes and aldoximes), and their structures were characterized by X-ray crystallography. Moreover, a simple and effective method for S-H insertion reactions of thiols was also developed, delivering the desired C-S bond products with good to excellent yields. It is worth noting that the efficacy of the developed methodology could be further shown by the expeditious synthesis of the PPAR agonist MBX-102 acid.

Safety of 3-(Trifluoromethyl)phenol. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Zhang, ZP; He, ZQ; Xie, YX; He, TT; Fu, YF; Yu, Y; Huang, F 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

Final Thoughts on Chemistry for 98-17-9

Recommanded Product: 3-(Trifluoromethyl)phenol. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Taira, J; Umei, T; Inoue, K; Kitamura, M; Berenger, F; Sacchettini, JC; Sakamoto, H; Aoki, S or concate me.

Recommanded Product: 3-(Trifluoromethyl)phenol. Taira, J; Umei, T; Inoue, K; Kitamura, M; Berenger, F; Sacchettini, JC; Sakamoto, H; Aoki, S in [Taira, Junichi; Umei, Tomohiro; Inoue, Keitaro; Berenger, Francois; Sakamoto, Hiroshi; Aoki, Shunsuke] Kyushu Inst Technol, Grad Sch Comp Sci & Syst Engn, Dept Biosci & Bioinformat, Iizuka, Fukuoka 8208502, Japan; [Kitamura, Mitsuru] Kyushu Inst Technol, Dept Appl Chem, 1-1 Sensui Cho, Kitakyushu, Fukuoka 8048550, Japan; [Sacchettini, James C.] Texas A&M Univ, Dept Biochem & Biophys, College Stn, TX 77843 USA published Improvement of the novel inhibitor for Mycobacterium enoyl-acyl carrier protein reductase (InhA): a structure-activity relationship study of KES4 assisted by in silico structure-based drug screening in , Cited 31. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9.

InhA or enoyl-acyl carrier protein reductase of Mycobacterium tuberculosis (mtInhA), which controls mycobacterial cell wall construction, has been targeted in the development of antituberculosis drugs. Previously, our in silico structure-based drug screening study identified a novel class of compounds (designated KES4), which is capable of inhibiting the enzymatic activity of mtInhA, as well as mycobacterial growth. The compounds are composed of four ring structures (A-D), and the MD simulation predicted specific interactions with mtInhA of the D-ring and methylene group between the B-ring and C-ring; however, there is still room for improvement in the A-ring structure. In this study, a structure-activity relationship study of the A-ring was attempted with the assistance of in silico docking simulations. In brief, the virtual chemical library of A-ring-modified KES4 was constructed and subjected to in silico docking simulation against mtInhA using the GOLD program. Among the selected candidates, we achieved synthesis of seven compounds, and the bioactivities (effects on InhA activity and mycobacterial growth and cytotoxicity) of the synthesized molecules were evaluated. Among the compounds tested, two candidates (compounds 3d and 3f) exhibited superior properties as mtInhA-targeted anti-infectives for mycobacteria than the lead compound KES4.

Recommanded Product: 3-(Trifluoromethyl)phenol. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Taira, J; Umei, T; Inoue, K; Kitamura, M; Berenger, F; Sacchettini, JC; Sakamoto, H; Aoki, 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

Discovery of 4-Hydroxyquinolin-2(1H)-one

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.. Formula: C9H7NO2

An article Novel Pyrazoloquinolin-2-ones: Design, synthesis, docking studies, and biological evaluation as antiproliferative EGFR-TK inhibitors WOS:000479184600037 published article about FACTOR RECEPTOR KINASE; SUBSTITUTED QUINOLINONES; PYRAZOLE DERIVATIVES; POTENTIAL ANTICANCER; ERLOTINIB; CANCER; CRIZOTINIB; CHEMISTRY; ASSAY in [Elbastawesy, Mohammed A., I; Ramadan, Mohamed] Al Azhar Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Assiut 71524, Egypt; [Aly, Ashraf A.] Menia Univ, Fac Sci, Dept Chem, Al Minya 61519, Egypt; [Elshaier, Yaseen A. M. M.] Univ Sadat City, Fac Pharm, Dept Organ & Med Chem, Menoufia 32958, Egypt; [Youssif, Bahaa G. M.] Assiut Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Assiut 71526, Egypt; [Brown, Alan B.] Florida Inst Technol, Program Chem, Melbourne, FL 32901 USA; [Abuo-Rahma, Gamal El-Din A.] Menia Univ, Fac Pharm, Dept Med Chem, Al Minya 61519, Egypt in 2019, Cited 50. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3. Formula: C9H7NO2

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.

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.. Formula: 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

What kind of challenge would you like to see in a future of compound:3,4-Dimethoxybenzaldehyde

COA of Formula: C9H10O3. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Bodaghifard, MA; Safari, S or concate me.

COA of Formula: C9H10O3. Authors Bodaghifard, MA; Safari, S in TAYLOR & FRANCIS LTD published article about in [Bodaghifard, Mohammad Ali; Safari, Somayeh] Arak Univ, Fac Sci, Dept Chem, Arak 3815688138, Iran; [Bodaghifard, Mohammad Ali] Arak Univ, Inst Nanosci & Nanotechnol, Arak, Iran in 2021.0, Cited 57.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

The significant stability of magnetic core and – OH functional groups on the surface of silica-coated cobalt ferrite (CoFe2O4@SiO2) nanoparticles make it a good candidate for functionalization and catalytic application. In this work, a surface-modified magnetic solid support with Cu(II) complex was prepared. The structure of the new nanostructure was characterized by Fourier-transform infrared spectroscopy (FT-IR), X-ray powder diffraction (XRD), thermogravimetric analysis (TGA/DTG), vibrating sample magnetometer (VSM), the field emission scanning electron microscopy (FE-SEM), the electron-dispersive X-ray spectroscopy (EDS), and inductively coupled plasma optical emission spectrometry (ICP/OES) techniques. The catalytic activity of the prepared hybrid nanomaterial was evaluated in the synthesis of 2,3-dihydroquinazolin-4(1H)-ones and high yields of desired products were obtained with green media. Some advantages of this method are high yields, short reaction times, green solvent and conditions, easy workup procedure, negligible copper leaching, reusability without a significant diminish in catalytic efficiency and simple separation of nanocatalyst by using an external magnet alongside the environmental compatibility and sustainability.

COA of Formula: C9H10O3. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Bodaghifard, MA; Safari, 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

Interesting scientific research on 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.. HPLC of Formula: C9H7NO2

HPLC of Formula: C9H7NO2. I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article 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 published in 2019, Reprint Addresses Aly, AA (corresponding author), Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt.; Kaoud, TS (corresponding author), Univ Texas Austin, Div Chem Biol & Med Chem, Austin, TX 78712 USA.. The CAS is 86-95-3. Through research, I have a further understanding and discovery of 4-Hydroxyquinolin-2(1H)-one.

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.

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.. HPLC of Formula: 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