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I found the field of Chemistry very interesting. Saw the article 4-Hydroxy-3-methyl-2(1H)-quinolone, originally discovered from a Brassicaceae plant, produced by a soil bacterium of the genus Burkholderia sp.: determination of a preferred tautomer and antioxidant activity published in 2020. Safety of 4-Hydroxyquinolin-2(1H)-one, Reprint Addresses Igarashi, Y (corresponding author), Toyama Prefectural Univ, Biotechnol Res Ctr, 5180 Kurokawa, Imizu, Toyama 9390398, Japan.; Igarashi, Y (corresponding author), Toyama Prefectural Univ, Dept Biotechnol, 5180 Kurokawa, Imizu, Toyama 9390398, Japan.. The CAS is 86-95-3. Through research, I have a further understanding and discovery of 4-Hydroxyquinolin-2(1H)-one

4-Hydroxy-3-methyl-2(1H)-quinolone (1), a molecule known for a long time and recently discovered from a Brassicaceae plant Isatis tinctoria without providing sufficient evidence to support the structure, was isolated from a fermentation extract of Burkholderia sp. 3Y-MMP isolated from a soil by a Zn2+ enrichment culture. Detailed spectroscopic analyses by MS and NMR, combined with C-13 chemical shift comparison with literature values of the related compounds and a synthetic preparation of 1, allowed its first full NMR characterization and identification of 2-quinolone but not 2-quinolinol (2) as the preferred tautomer for this heterocyclic system. While the metal-chelating activity was negligible, compound 1 at 10 mu M, a concentration lower than that in liquid production cultures, quenched hydroxy radical-induced chemiluminescence emitted by luminol by 86%. Because some Burkholderia species are pathogenic to plants and animals, the above result suggests that 1 is a potential antioxidant to counteract reactive oxygen species-based immune response in the host organisms.

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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

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Quality Control of 4-Hydroxyquinolin-2(1H)-one. In 2019 ORG LETT published article about ERIOSTEMON; SYNTHASE in [Coleman, Matthew A.; Burchill, Laura; Sumby, Christopher J.; George, Jonathan H.] Univ Adelaide, Dept Chem, Adelaide, SA 5005, Australia in 2019, Cited 12. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3.

The structure of furoerioaustralasine, a unique Australian alkaloid, has been revised based on a concise, biomimetic synthesis. The key step is a stereospecific, intramolecular ring opening of an epoxide to form a central dihydrofuran fused to a quinoline ring system.

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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

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Welcome to talk about 86-95-3, If you have any questions, you can contact Elbastawesy, MAI; Aly, AA; Ramadan, M; Elshaier, YAMM; Youssif, BGM; Brown, AB; Abuo-Rahma, GEDA or send Email.. Computed Properties of 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. Computed Properties of 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.

Welcome to talk about 86-95-3, If you have any questions, you can contact Elbastawesy, MAI; Aly, AA; Ramadan, M; Elshaier, YAMM; Youssif, BGM; Brown, AB; Abuo-Rahma, GEDA or send Email.. 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

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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. SDS of cas: 86-95-3. 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.

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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

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SDS of cas: 86-95-3. Welcome to talk about 86-95-3, If you have any questions, you can contact Chheda, PR; Kummer, DA; Nishimura, RT; McClure, KJ; Venkatesan, H or send Email.

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. SDS of cas: 86-95-3. 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.

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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

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Authors Aly, AA; El-Sheref, EM; Bakheet, MEM; Mourad, MAE; Brase, S; Ibrahim, MAA; Nieger, M; Garvalov, BK; Dalby, KN; Kaoud, TS in ACADEMIC PRESS INC ELSEVIER SCIENCE published article about ACQUIRED-RESISTANCE; IN-VITRO; PROTEIN; DISCOVERY; DOCKING; PHOSPHORYLATION; ACTIVATION; PRODUCTS; QUINONES; BVD-523 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 in 2019, Cited 57. Application In Synthesis of 4-Hydroxyquinolin-2(1H)-one. 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.

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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

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Product Details of 86-95-3. 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.

Product Details of 86-95-3. Welcome to talk about 86-95-3, If you have any questions, you can contact Chheda, PR; Kummer, DA; Nishimura, RT; McClure, KJ; Venkatesan, H 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

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An article Catalyst-Solvent System for PASE Approach to Hydroxyquinolinone-Substituted Chromeno[2,3-b]pyridines Its Quantum Chemical Study and Investigation of Reaction Mechanism WOS:000553858800110 published article about STEP ECONOMY PASE; ONE-POT; CORROSION-INHIBITORS; MULTICOMPONENT REACTIONS; ORGANIC-SYNTHESIS; MILD-STEEL; PARTITION-COEFFICIENTS; ATOM ECONOMY; EFFICIENT; DERIVATIVES in [Ryzhkov, Fedor, V; Ryzhkova, Yuliya E.; Elinson, Michail N.; Fakhrutdinov, Artem N.; Vereshchagin, Anatoly N.; Egorov, Mikhail P.] Russian Acad Sci, ND Zelinsky Inst Organ Chem, Leninsky Pr 47, Moscow 119991, Russia; [Vorobyev, Stepan V.] Gubkin Russian State Univ Oil & Gas, Dept Organ Chem & Petr Chem, 65 Leninsky Prospect, Moscow 119991, Russia in 2020, Cited 63. Quality Control of 4-Hydroxyquinolin-2(1H)-one. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3

The Pot, Atom, and Step Economy (PASE) approach is based on the Pot economy principle and unites it with the Atom and Step Economy strategies; it ensures high efficiency, simplicity and low waste formation. The PASE approach is widely used in multicomponent chemistry. This approach was adopted for the synthesis of previously unknown hydroxyquinolinone substituted chromeno[2,3-b]pyridines via reaction of salicylaldehydes, malononitrile dimer and hydroxyquinolinone. It was shown that an ethanol-pyridine combination is more beneficial than other inorganic or organic catalysts. Quantum chemical studies showed that chromeno[2,3-b]pyridines has potential for corrosion inhibition. Real time H-1 NMR monitoring was used for the investigation of reaction mechanism and 2-((2H-chromen-3-yl)methylene)malononitrile was defined as a key intermediate in the reaction.

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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

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An article Synthesis of New Fused Heterocyclic 2-Quinolones and 3-Alkanonyl-4-Hydroxy-2-Quinolones WOS:000496249500151 published article about FLUOROQUINOLONES; DERIVATIVES; INHIBITORS; MECHANISM; DESIGN; SIGNAL 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 in 2019, Cited 31. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3. Quality Control of 4-Hydroxyquinolin-2(1H)-one

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.

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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

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Welcome to talk about 86-95-3, 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 send Email.. Name: 4-Hydroxyquinolin-2(1H)-one

Name: 4-Hydroxyquinolin-2(1H)-one. 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.

Welcome to talk about 86-95-3, 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 send Email.. Name: 4-Hydroxyquinolin-2(1H)-one

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