Tag: M.W=150-200

Recently I am researching about BIOLOGICAL EVALUATION; ANTITUMOR-ACTIVITY; DERIVATIVES BEARING; MULTIKINASE INHIBITOR; CLICK CHEMISTRY; DESIGN; CANCER; DISCOVERY; MOIETY; METASTASIS, Saw an article supported by the Institute for the Promotion of Teaching Science and Technology (IPST) [19/2558]; The Thailand Research FundThailand Research Fund (TRF) [RTA6280004]; Department of Chemistry, Faculty of Science, Silpakorn University; Center of Excellence in Hepatitis and Liver Cancer, Department of Biochemistry, Faculty of Medicine, Chulalongkorn University. Published in ACADEMIC PRESS INC ELSEVIER SCIENCE in SAN DIEGO ,Authors: Palakhachane, S; Ketkaew, Y; Chuaypen, N; Sirirak, J; Boonsombat, J; Ruchirawat, S; Tangkijvanich, P; Suksamrarn, A; Limpachayaporn, P. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol. Category: indole-building-block

A series of 1,2,3-triazole-containing Sorafenib analogues, in which the aryl urea moiety of Sorafenib (1) was replaced with a 1,2,3-triazole ring linking a substituted phenoxy fragment, were prepared successfully via Huisgen 1,3-dipolar cycloaddition and nucleophilic aromatic substitution. The studies of cytotoxicity towards human hepatocellular carcinoma (HCC) cell lines, HepG2 and Huh7, indicated that p-tert-butylphenoxy analogue 2m showed significant inhibitory activity against Huh7 with IC50 = 5.67 +/- 0.57 mu M. More importantly, 2m showed low cytotoxicity against human embryonal lung fibroblast cell line, MRC-5, with IC50 > 100 mu M, suggesting its highly selective cytotoxic activity (SI > 17.6) towards Huh7 which is much superior to that of Sorafenib (SI = 6.73). The molecular docking studies revealed that the analogue 2m bound B-RAF near the binding position of Sorafenib, while it interacted VEGFR2 efficiently at the same binding position of Sorafenib. However, 2m exhibited moderate inhibitory activity toward B-RAF, implying that its anti-Huh7 effect might not strictly relate to inhibition of B-RAF. Wound healing and BrdU cell proliferation assays confirmed anti-cell migration and anti-cell proliferative activities towards Huh7. With its inhibitory efficiency and high safety profile, 2m has been identified as a promising candidate for the treatment of HCC.

Category: indole-building-block. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Palakhachane, S; Ketkaew, Y; Chuaypen, N; Sirirak, J; Boonsombat, J; Ruchirawat, S; Tangkijvanich, P; Suksamrarn, A; Limpachayaporn, P 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

Category: indole-building-block. Recently I am researching about Z ISOMERIZATION; ATOM ECONOMY; IONIC LIQUID; COUMARINS; BIOSYNTHESIS; DERIVATIVES; ALKYNOATES, Saw an article supported by the WWU Munster; CiM-IMPRS Graduate School. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Nevesely, T; Daniliuc, CG; Gilmour, R. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol

An operationally simple one-pot protocol has been developed to enable the conversion of diversely substituted cinnamic acid derivatives into angularly-fused dihydrocoumarins (up to 94%). Inspired by coumarin biosynthesis, this reaction cascade harnesses photochemical E -> Z alkene isomerization enabled by energy transfer catalysis using inexpensive thioxanthen-9-one (TX) under irradiation at 402 nm. Subsequent lactonization generates the heterocyclic core prior to a second photosensitization event to induce a [2 + 2] cycloaddition, again mediated by TX. The tetracyclic products are generated efficiently, and proof of the structure was established by X-ray crystallography. Mechanistic investigations, including structural probes and NMR reaction monitoring, support the postulated order of events. The study underscores the synthetic value of inexpensive small-molecule organic photocatalysts in the generation of structural complexity via sequential pi-bond activation.

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Nevesely, T; Daniliuc, CG; Gilmour, R 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

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

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

Computed Properties of 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.

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 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 2019 CHEM-EUR J published article about NICKEL-CATALYZED AMINATION; CROSS-COUPLING REACTIONS; LONG-LIVED CATALYSTS; ONE-POT CONVERSION; C-H AMINATION; ARYL MIGRATION; AROMATIC-COMPOUNDS; METAL; CLEAVAGE; COPPER in [Lardy, Samuel W.; Luong, Kristine C.; Schmidt, Valerie A.] Univ Calif San Diego, Dept Chem & Biochem, 9500 Gilman Dr, La Jolla, CA 92093 USA in 2019, Cited 75. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9. Category: indole-building-block

Phenolic, lignin-derived substrates have emerged as desirable biorenewable chemical feedstocks for coupling reactions. A radical-mediated conversion of phenol derivatives to anilines is reported, using unfunctionalized hydroxamic acids as the N-centered radical source. The applicability of this triethyl phosphite mediated O-atom transfer approach, which tolerates a range of steric and electronic demands to naturally occurring phenols and lignin models, has been demonstrated in this work to access the corresponding aniline derivatives.

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Lardy, SW; Luong, KC; Schmidt, VA 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

Formula: C9H7NO2. Recently I am researching about MICROBIAL-PRODUCTION; SALICYLATE BIOSYNTHESIS; PURIFICATION; ENZYME, Saw an article supported by the National Research Foundation – Ministry of Education, Science and Technology [NRF-2019R1A2C1002714]; Next-Generation BioGreen 21 Program, Ministry of Education, Science and Technology, Republic of Korea [PJ01326001]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Choo, HJ; Ahn, JH. 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.

Formula: C9H7NO2. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Choo, HJ; Ahn, JH 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

Formula: C9H10O3. Authors Reihani, N; Kiyani, H in BENTHAM SCIENCE PUBL LTD published article about in [Reihani, Neda; Kiyani, Hamzeh] Damghan Univ, Sch Chem, POB 36716-41167, Damghan, Iran; [Kiyani, Hamzeh] Shahrekord Univ, Fac Sci, Dept Chem, Shahrekord, Iran in 2021.0, Cited 67.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

An efficient synthesis of 4-arylidene-3-alkylisoxazole-5(4H)-ones has been implemented via the three-component cyclocondensation of aryl(heteroaryl)aldehydes with hydroxylamine hydrochloride and beta-ketoesters. The potassium 2,5-dioxoimidazolidin-1-ide has been introduced as the new organocatalyst to facilitate this heterocyclization. In the current process, three starting materials, including substituted benzaldehydes/heterocyclic aromatic aldehydes, hydroxylamine hydrochloride, and ethyl acetoacetate/propyl acetoacetate/butyryl acetoacetate have been successfully used to synthesize the number of substituted isoxazole-5-(4H)-ones in good to high yields in ethylene glycol as a green reaction medium at 80 degrees C. The low catalyst loading is also a main advantage over some reported catalysts.

About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Reihani, N; Kiyani, H or concate me.. 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

Category: indole-building-block. In 2021.0 ORG LETT published article about ENANTIOSELECTIVE CONSTRUCTION; VINYLETHYLENE CARBONATES; NAZAROV CYCLIZATION; BOND; DESYMMETRIZATION; HETEROCYCLES; REACTIVITY; ALCOHOL; CENTERS; SYSTEM in [Yang, Biwei; Zuo, Linhong; Chang, Xiaowei; Liu, Teng; Cui, Manying; Liu, Yang; Sun, Haiyu; Chen, Weipeng; Guo, Wusheng] Xi An Jiao Tong Univ, Frontier Inst Sci & Technol FIST, Xian 710045, Peoples R China in 2021.0, Cited 71.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9.

A decarboxylative protocol has been developed toward a range of carbocycles. The key success is based on the use of a batch of newly designed cyclic carbonates as substrates that can provide carbon-carbon zwitterion intermediate under palladium catalysis. The kinetics of the reactions are controllable toward either strained seven- or thermodynamically more favored five-membered carbocycles. The release of this chemistry will shed light on the synthesis of complex and valuable cyclic structures.

About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Yang, BW; Zuo, LH; Chang, XW; Liu, T; Cui, MY; Liu, Y; Sun, HY; Chen, WP; Guo, WS 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

Computed Properties of C9H7NO2. 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.

Computed Properties of C9H7NO2. 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.

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 Engineering; Materials Science very interesting. Saw the article A novel method of temporary solidification and extraction of underwater fragile relics in their original state published in 2021.0. COA of Formula: C9H10O3, Reprint Addresses Zhang, BJ (corresponding author), Zhejiang Univ, Dept Cultural Heritage & Museol, Hangzhou 310028, Peoples R China.. The CAS is 120-14-9. Through research, I have a further understanding and discovery of 3,4-Dimethoxybenzaldehyde

Fragile cultural relics at underwater archaeological sites are difficult to preserve in situ over long time periods due to the effects of a complex and constantly changing surrounding environment. Thus, extracting the relics from water and preserving them in a controllable environment is of primary importance. In this paper, the technology of temporary reinforcement and extraction of underwater fragile relics with veratraldehyde followed by a process of secondary temporary reinforcement using polyethylene glycol (PEG) was studied. After investigating the melting temperature and permeability of PEGs with different molecular weights, we found that PEG-3000 is an excellent candidate as the secondary reinforcing agent for the extracted relics. In the laboratory, combined with veratraldehyde and polypropylene-fiber cloth as temporary underwater strengthening materials, and selected dispersed beaded jewelry and a broken three-dimensional crock as our research subject, we carried out an entire retrieval process-temporary stabilization and secondary temporary reinforcement, to systematically evaluate the technological aspects of safely excavating fragile underwater relics in the original state. After being extracted from water and subjected to secondary temporary reinforcement using PEG-3000, the beaded jewelry and broken crock retained their underwater shape and arrangement completely. The use of secondary reinforcing agent prevents the removal process of veratraldehyde and enclosed sediment from affecting the state of the relics.

About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Chen, XQ; Zhang, BJ; Zhang, ZG or concate me.. 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