Tag: M.W=150-200

Computed Properties of C9H7NO2. In 2019 BIOORG CHEM 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. 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.

Computed Properties of C9H7NO2. 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

I found the field of Chemistry very interesting. Saw the article Visible-Light-Induced Radical Carbo-Cyclization/gem-Diborylation through Triplet Energy Transfer between a Gold Catalyst and Aryl Iodides published in 2020. Safety of 3-(Trifluoromethyl)phenol, Reprint Addresses Hashmi, ASK (corresponding author), Heidelberg Univ, Organ Chem Inst, D-69120 Heidelberg, Germany.; Hashmi, ASK (corresponding author), King Abdulaziz Univ KAU, Fac Sci, Chem Dept, Jeddah 21589, Saudi Arabia.. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol

Geminal diboronates have attracted significant attention because of their unique structures and reactivity. However, benzofuran-, indole-, and benzothiophene-based benzylic gem-diboronates, building blocks for biologically relevant compounds, are unknown. A promising protocol using visible light and aryl iodides for constructing valuable building blocks, including benzofuran-, indole-, and benzothiophene-based benzylic gem-diboronates, via radical carbo-cyclization/gem-diborylation of alkynes with a high functional group tolerance is presented. The utility of these gem-diboronates has been demonstrated by a 10 g scale conversion, by versatile transformations, by including the synthesis of approved drug scaffolds and two approved drugs, and even by polymer synthesis. The mechanistic investigation indicates that the merging of the dinuclear gold catalyst (photoexcitation by 315-400 nm UVA light) with Na2CO3 is directly responsible for photosensitization of aryl iodides (photoexcitation by 254 nm UV light) with blue LED light (410-490 nm, lambda(max) = 465 nm) through an energy transfer (EnT) process, followed by homolytic cleavage of the C-I bond in the aryl iodide substrates.

Safety of 3-(Trifluoromethyl)phenol. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Zhang, LM; Si, XJ; Rominger, F; Hashmi, ASK 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 Awasthi, A; Yadav, P; Tiwari, DK in ROYAL SOC CHEMISTRY published article about in [Awasthi, Annapurna; Yadav, Pushpendra; Tiwari, Dharmendra Kumar] Ctr Biomed Res CBMR, Mol Synth & Drug Discovery Unit, SGPGIMS Campus,Raibareli Rd, Lucknow 226014, Uttar Pradesh, India; [Awasthi, Annapurna; Yadav, Pushpendra] Banaras Hindu Univ, Inst Sci, Dept Chem, Varanasi 221005, Uttar Pradesh, India in 2021.0, Cited 63.0. HPLC of Formula: C9H10O3. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

An efficient, general, and practical route for highly diastereoselective synthesis of aza-spirocyclic pyrazolones from easily available alpha-amino acids, aldehydes, and alkylidene pyrazolones by means of a decarboxylative annulation process is reported. This high-yielding reaction proceeds through a [3+2]-cycloaddition reaction between alkylidene pyrazolones and a nonstabilized azomethine ylide generated in situ. This method provides easy and smooth access to a variety of highly functionalized aza-spirocyclic pyrazolones in excellent yields (up to 96%). The obtained spiro-pyrazolones comprise four contiguous stereogenic centers including a quaternary carbon center.

About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Awasthi, A; Yadav, P; Tiwari, DK or concate me.. HPLC 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

SDS of cas: 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.

About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Chheda, PR; Kummer, DA; Nishimura, RT; McClure, KJ; Venkatesan, H or concate me.. SDS of cas: 86-95-3

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 Agriculture; Chemistry; Food Science & Technology very interesting. Saw the article Synthesis of Three Bioactive Aromatic Compounds by Introducing Polyketide Synthase Genes into Engineered Escherichia coli published in 2019. Application In Synthesis of 4-Hydroxyquinolin-2(1H)-one, Reprint Addresses Ahn, JH (corresponding author), Konkuk Univ, Bio Mol Informat Ctr, Dept Biosci & Biotechnol, Seoul 05029, South Korea.. The CAS is 86-95-3. Through research, I have a further understanding and discovery of 4-Hydroxyquinolin-2(1H)-one

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.

About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Choo, HJ; Ahn, JH or concate me.. Application In Synthesis of 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

Recently I am researching about ALZHEIMERS-DISEASE; A-BETA; CHEMICAL-SYNTHESIS; DESIGN; ABAD/17-BETA-HSD10; IDENTIFICATION; OPTIMIZATION; DERIVATIVES; CHEMISTRY; PEPTIDE, Saw an article supported by the Merck Sharpe & Dome e Faculte de medecine (Universite Laval); Mitacs Inc (Montreal, QC, Canada); foundation of CHU de Quebec (Endocrinology and Nephrology Unit); Faculty of Medicine of Universite Laval. Category: indole-building-block. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Boutin, S; Maltais, R; Roy, J; Poirier, D. The CAS is 120-14-9. Through research, I have a further understanding and discovery of 3,4-Dimethoxybenzaldehyde

17beta-Hydroxysteroid dehydrogenase type 10 (17 beta-HSD10) is the only mitochondrial member of 17 beta-HSD family. This enzyme can oxidize estradiol (E2) into estrone (E1), thus reducing concentration of this neuroprotective steroid. Since 17 beta-HSD10 possesses properties that suggest a possible role in Alzheimer’s disease, its inhibition appears to be a therapeutic strategy. After we identified the androsterone (ADT) derivative 1 as a first steroidal inhibitor of 17 beta-HSD10, new analogs were synthesized to increase the metabolic stability, to improve the selectivity of inhibition over 17 beta-HSD3 and to optimize the inhibitory potency. From six D-ring derivatives of 1 (17-C = O), two compounds (17 beta-H/17 alpha-OH and 17 beta-OH/17aC CH) were more metabolically stable and did not inhibit the 17 beta-HSD3. Moreover, solid phase synthesis was used to extend the molecular diversity on the 3b-piperazinylmethyl group of the steroid base core. Eight over 120 new derivatives were more potent inhibitors than 1 for the transformation of E2 to E1, with the 4-(4-trifluoromethyl-3-methoxybenzyl)piperazin-1-ylmethyl-ADT (D-3,7) being 16 times more potent (IC50 = 0.14 mM). Finally, D-ring modification of D-3,7 provided 17 beta-OH/17 alpha-C CH derivative 25 and 17 beta-H/17 alpha-OH derivative 26, which were more potent inhibitor than 1 (1.8 and 2.4 times, respectively). (C) 2020 Elsevier Masson SAS. All rights reserved.

About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Boutin, S; Maltais, R; Roy, J; Poirier, D 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

An 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 WOS:000548343000001 published article about 2,4-DIHYDROXYQUINOLINE; DERIVATIVES; QUINOLINE; ANALOGS in [Li, Dandan; Oku, Naoya; Igarashi, Yasuhiro] Toyama Prefectural Univ, Biotechnol Res Ctr, 5180 Kurokawa, Imizu, Toyama 9390398, Japan; [Li, Dandan; Oku, Naoya; Igarashi, Yasuhiro] Toyama Prefectural Univ, Dept Biotechnol, 5180 Kurokawa, Imizu, Toyama 9390398, Japan; [Shinozaki, Yukiko] Toyama Coll, Natl Inst Technol, 13 Hongo Machi, Toyama, Toyama 9398630, Japan; [Kurokawa, Yoichi] Fukui Prefectural Univ, Dept Biosci & Biotechnol, Eiheiji Cho, Fukui, Japan in 2020, Cited 45. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3. Recommanded Product: 86-95-3

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.

About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Li, DD; Oku, N; Shinozaki, Y; Kurokawa, Y; Igarashi, Y or concate me.. Recommanded Product: 86-95-3

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 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. COA of Formula: C9H7NO2, 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.

COA of Formula: C9H7NO2. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Li, DD; Oku, N; Shinozaki, Y; Kurokawa, Y; Igarashi, Y 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

In 2020 ORG LETT published article about INSERTION in [Empel, Claire; Jana, Sripati; Pei, Chao; Koenigs, Rene M.] Rhein Westfal TH Aachen, Inst Organ Chem, D-52074 Aachen, Germany; [Empel, Claire; Thanh Vinh Nguyen; Koenigs, Rene M.] Univ New South Waley, Sch Chem, Sydney, NSW 2052, Australia in 2020, Cited 44. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9. Product Details of 98-17-9

In this work, we report a thorough investigation of the reaction of phenols with aryldiazoacetates. Mechanistic studies using different spectroscopic methods and theoretical calculations suggest a hydrogen bond between phenol and aryldiazoacetates, which can be modulated by the phenol acidity. The pK(A) of phenol and therefore the hydrogen bond plays an important role in a subsequent photoinduced proton transfer reaction to give the formal O-H functionalization product of phenols.

Product Details of 98-17-9. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Empel, C; Jana, S; Pei, C; Nguyen, TV; Koenigs, RM or concate me.

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

An article Catalyst-free visible-light induced synthesis of nitrogen- and oxygen-containing heterocycles from 1,3-diketones WOS:000604195100001 published article about ONE-POT SYNTHESIS; POLYHYDROQUINOLINE DERIVATIVES; ORGANIC-SYNTHESIS; CHEMISTRY in [Chen, Lu; Lin, Zhenyuan; Zhang, Xuefang; Tan, Leshi; Zhang, Min; Li, Yibiao] Wuyi Univ, Sch Biotechnol & Hlth Sci, Jiangmen, Peoples R China in 2021.0, Cited 40.0. Computed Properties of C9H10O3. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

The synthesis of nitrogen- and oxygen-containing heterocycles has found many applications in the preparation of biomedical intermediates, yet actual synthetic procedures display limitations such as high-loading catalysts, harsh reaction conditions and tedious preparation of heterogeneous catalysts. Alternatively, photocatalysis allows to access functional products with minimum synthetic procedures and waste generation. Here, we present an efficient, simple, green protocol for the synthesis of N- and O-containing six-membered-ring compounds under mild conditions under visible blue light. Various aldehydes and 1,3-diketones can be reacted to afford eight series of corresponding 1,4-dihydropyridines and 4H-benzo[b]pyrans. This protocol has some merits such as the use of abundant and sustainable aqueous ethanol as solvent, short reaction time (within 60 min), no need of catalyst and broad functional group tolerance to afford 81 different series of target molecules in 75-96% yield under mild conditions.

Computed Properties of C9H10O3. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Chen, L; Lin, ZY; Zhang, XF; Tan, LS; Zhang, M; Li, YB 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