Tag: M.W=150-200

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. Formula: C9H7NO2, 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.

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

I found the field of Chemistry very interesting. Saw the article Synthesis of ethanol from aryl methyl ether/lignin, CO2 and H-2 published in 2019. HPLC of Formula: C7H5F3O, Reprint Addresses Qian, QL; Han, BX (corresponding author), Chinese Acad Sci, CAS Key Lab Colloid Interface & Chem Thermodynam, CAS Res Educ Ctr Excellence Mol Sci, Beijing Natl Lab Mol Sci,Inst Chem, Beijing 100190, Peoples R China.; Han, BX (corresponding author), Univ Chinese Acad Sci, Sch Chem & Chem Engn, Beijing 100049, Peoples R China.; Qian, QL; Han, BX (corresponding author), Huairou Natl Comprehens Sci Ctr, Phys Sci Lab, 5 Yanqi East Second St, Beijing 101400, Peoples R China.; Han, BX (corresponding author), East China Normal Univ, Sch Chem & Mol Engn, Shanghai Key Lab Green Chem & Chem Proc, Shanghai 200062, Peoples R China.. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol

Currently, ethanol is produced via hydration of ethene or fermentation of foods. Lignin and CO2 are abundant, cheap and renewable feedstocks. Synthesis of ethanol using the lignin or its derivatives is of great importance, but is a great challenge and has rarely been reported. Herein, we propose a route to synthesize ethanol from CO2, H-2, and lignin or various aryl methyl ethers, which can be derived from lignin. The reaction could be effectively conducted using Ru-Co bimetallic catalyst and the TON of ethanol could reach 145. Interestingly, ethanol was the only liquid product when lignin was used. A series of control experiments indicate that ethanol was formed via cleavage of aryl ether bond, reverse water gas shift (RWGS) reaction, and C-C bond formation. This protocol opens a way to produce ethanol using abundant renewable resources.

HPLC of Formula: C7H5F3O. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Zhang, JJ; Qian, QL; Wang, Y; Bediako, BBA; Yan, J; Han, BX 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 Polyfluoroaromatic stavudine (d4T) ProTides exhibit enhanced anti-HIV activity WOS:000497964000013 published article about DERIVATIVES; NUCLEOSIDE; PHOSPHATE in [Kandil, Sahar; Chapman, Fiona M.; Westwell, Andrew D.; McGuigan, Christopher] Cardiff Univ, Sch Pharm & Pharmaceut Sci, King Edward VII Ave, Cardiff CF10 3NB, S Glam, Wales; [Pannecouque, Christophe] Katholieke Univ Leuven, Rega Inst Med Res, Lab Virol & Chemotherapy, Minderbroedersstr 10, B-3000 Leuven, Belgium in 2019, Cited 17. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9. Recommanded Product: 98-17-9

Human Immunodeficiency Virus (HIV) damages the immune system and leads to the life-threatening acquired immunodeficiency syndrome (AIDS). Despite the advances in the field of antiretroviral treatment, HIV remains a major public health challenge. Nucleosides represent a prominent chemotherapeutic class for treating viruses, however their cellular uptake, kinase-mediated activation and catabolism are limiting factors. Herein, we report the synthesis and in vitro evaluation of stavudine (d4T) ProTides containing polyfluorinated aryl groups against two strains; HIV-1 (IIIB) and HIV-2 (ROD). ProTide 5d containing a meta-substituted pentafluorosulfanyl (3-SF5) aryl group showed superior antiviral activity over the parent d4T and the nonfluorinated analogue 5a. ProTide 5d has low nano-molar antiviral activity; (IC50=30 nM, HIV-1) and (IC50=36 nM, HIV-2) which is over tenfold more potent than d4T. Interestingly, ProTide 5d showed a significantly high selectivity indices with SI=1753 (HIV-1) and 1461 (HIV-2) which is more than twice that of the d4T. All ProTides were screened in wild type as well as thymidine kinase deficient (TK-) cells. Enzymatic activation of ProTide 5d using carboxypeptidase Y enzyme and monitored using both P-31 and F-19 NMR is presented.

Recommanded Product: 98-17-9. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Kandil, S; Pannecouque, C; Chapman, FM; Westwell, AD; McGuigan, C 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

Safety of 3,4-Dimethoxybenzaldehyde. I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article 3,7-bis-benzylidene hydrazide ciprofloxacin derivatives as promising antiproliferative dual TOP I & TOP II isomerases inhibitors published in 2021, Reprint Addresses Abdel-Aziz, M (corresponding author), Menia Univ, Fac Pharm, Dept Med Chem, Al Minya 61519, Egypt.; Abuo-Rahma, GEDA (corresponding author), Deraya Univ, Fac Pharm, Dept Pharmaceut Chem, New Minia, Minia, Egypt.. The CAS is 120-14-9. Through research, I have a further understanding and discovery of 3,4-Dimethoxybenzaldehyde.

We report herein design and synthesis of a new series of 3,7-bis-benzylidenes of ciprofloxacin. Most of the target compounds revealed good cytotoxic activity; the most potent 4e and 4i achieved strong broad spectrum antiproliferative activity with comparable activity to Doxorubicin with IC50 (M-mu) of 1.21 +/- 0.02, 0.87 +/- 0.04, 1.21 +/- 0.02; 0.41 +/- 0.02, 0.57 +/- 0.06, 1.31 +/- 0.04 and 1.26 +/- 0.01, 1.79 +/- 0.04, 0.63 +/- 0.01 against leukemia cancer cell line HL-60 (TB), colon cancer cell line HCT-116 and breast cancer cell line MCF7, respectively. Moreover, the most potent derivative 4i induced apoptosis at G2/M phase Investigating the mechanism of action of compounds 4e, 4 h and 4i exhibited promising dual TOP I alpha and TOP IIB % inhibition comparable to Camptothecin and Etoposide; respectively. Docking of 4e, 4 h and 4i into the active site of topo I and II proteins compared to Camptothein and Etoposide revealed acceptable binding score and augmented enzyme assay data. Hence, 4e and 4i are promising targeted antiproliferative dual acting TOP I alpha TOP IIB inhibitors that require further optimization.

Safety of 3,4-Dimethoxybenzaldehyde. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Samir, M; Ramadan, M; Abdelrahman, MH; Abdelbaset, MS; Abourehab, MAS; Abdel-Aziz, M; Abuo-Rahma, GEDA 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 Host RNA quality control as a hepatitis B antiviral target WOS:000657774400001 published article about NONCANONICAL POLY(A) POLYMERASE; POLYADENYLATION SIGNAL; MOLECULAR-BIOLOGY; STEM-LOOP; VIRUS; DEGRADATION; EXOSOME; TRAMP; DECAY; TRANSCRIPTS in [Block, Timothy M.; Zhou, Tianlun] Baruch S Blumberg Inst, Doylestown, PA 18902 USA; [Young, John A. T.] F Hoffmann La Roche Ltd, Roche Innovat Ctr Basel, Roche Pharma Res & Early Dev, Basel, Switzerland; [Javanbakht, Hassan] SQZ Biotechnol, 200 Arsenal Yards Blvd,Suite 210, Watertown, MA 02472 USA; [Sofia, Michael J.] Arbutus Biopharma Inc, 701 Vet Circle, Warminster, PA 18974 USA in 2021, Cited 69. Name: 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

Inhibition of the host RNA polyadenylating polymerases, PAPD5 and PAPD7 (PAPD5/7), with dihydroquinolizinone, a small orally available, molecule, results in a rapid and selective degradation of hepatitis B virus (HBV) RNA, and hence reduction in the amounts of viral gene products. DHQ, is a first in class investigational agent and could represent an entirely new category of HBV antivirals. PAPD5 and PAPD7 are noncanonical, cell specified, polyadenylating polymerases, also called terminal nucleotidyl transferases 4B and 4A (TENT4B/A), respectively. They are involved in the degradation of poor-quality cell transcripts, mostly noncoding RNAs and in the maturation of a sub-set of transcripts. They also appear to play a role in shielding some mRNA from degradation. The results of studies with DHQ, along with other recent findings, provide evidence that repression of the PAPD5/7 arm of the cell RNA quality control pathway, causes a profound (multifold) reduction rather than increase, in the amount of HBV pre-genomic, pre-core and HBsAg mRNA levels in tissue culture and animal models, as well. In this review we will briefly discuss the need for new HBV therapeutics and provide background about HBV transcription. We also discuss cellular degradation of host transcripts, as it relates to a new family of anti-HBV drugs that interfere with these processes. Finally, since HBV mRNA maturation appears to be selectively sensitive to PAPD5/7 inhibition in hepatocytes, we discuss the possibility of targeting host RNA quality control as an antiviral strategy.

Name: 4-Hydroxyquinolin-2(1H)-one. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Block, TM; Young, JAT; Javanbakht, H; Sofia, MJ; Zhou, TL 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

Product Details of 120-14-9. Authors Chu, PC; Wu, YC; Chen, CY; Hung, YS; Chang, CS in FUTURE SCI LTD published article about in [Chu, Po-Chen] China Med Univ, Dept Cosmeceut, Taichung 40402, Taiwan; [Chu, Po-Chen] China Med Univ, Grad Inst Cosmeceut, Taichung 40402, Taiwan; [Chu, Po-Chen; Chang, Chih-Shiang] China Med Univ, Drug Dev Ctr, Taichung 40402, Taiwan; [Wu, Yu-Chieh; Chen, Chien-Yu; Hung, Yu-Syuan; Chang, Chih-Shiang] China Med Univ, Sch Pharm, Coll Pharm, Taichung 40402, Taiwan in 2021, Cited 35. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

Aim: Tumor cells adapt to hypoxic microenvironments by releasing the key transcription factor HIF-1 alpha, which promotes angiogenesis, glycolytic phenotype, metastasis and erythropoiesis, allowing proliferation amid low oxygen levels. Therefore, therapeutic targeting of HIF-1 alpha represents a viable strategy for cancer therapy. Methods & Results: The authors synthesized a series of novel tetrahydroquinazoline derivatives in six steps and demonstrated that their development had a unique ability to suppress HIF-1 alpha expression through proteasomal degradation. Conclusion: Among these compounds, CDMP-TQZ (8bf) exhibited the highest antiproliferative potency in human cancer cells, in part through downregulation of HIF-1 alpha.

About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Chu, PC; Wu, YC; Chen, CY; Hung, YS; Chang, CS or concate me.. Product Details of 120-14-9

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

Name: 4-Hydroxyquinolin-2(1H)-one. Recently I am researching about ACQUIRED-RESISTANCE; IN-VITRO; PROTEIN; DISCOVERY; DOCKING; PHOSPHORYLATION; ACTIVATION; PRODUCTS; QUINONES; BVD-523, Saw an article supported by the Cancer Prevention and Research Institute of Texas grant [RP160657]; National Institutes of HealthUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USA [R01 GM123252]; Welch FoundationThe Welch Foundation [F-1390]; Science and Technology Development Fund, STDF, EgyptScience and Technology Development Fund (STDF); NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCESUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USANIH National Institute of General Medical Sciences (NIGMS) [R01GM123252] Funding Source: NIH RePORTER. Published in ACADEMIC PRESS INC ELSEVIER SCIENCE in SAN DIEGO ,Authors: Aly, AA; El-Sheref, EM; Bakheet, MEM; Mourad, MAE; Brase, S; Ibrahim, MAA; Nieger, M; Garvalov, BK; Dalby, KN; Kaoud, TS. 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.

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

Quality Control of 4-Hydroxyquinolin-2(1H)-one. 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

Authors Marjani, AP; Khalafy, J; Farajollahi, A in WILEY 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. Product Details of 86-95-3. 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.

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

An article Direct Access for the Regio- and Stereoselective Synthesis of N-Alkenylpyrazoles and Chromenopyrazoles WOS:000618540600019 published article about ONE-POT SYNTHESIS; REGIOSELECTIVE SYNTHESIS; FACILE SYNTHESIS; PYRAZOLES; HYDRAZONES; ALKYNES; TOSYLHYDRAZONES; DERIVATIVES; HYDRAZIDES; COMPLEXES in [Kurma, Siva Hariprasad; Bhimapaka, China Raju] CSIR Indian Inst Chem Technol, Dept Organ Synth & Proc Chem, Hyderabad 500007, India; [Kurma, Siva Hariprasad; Bhimapaka, China Raju] Acad Sci & Innovat Res AcSIR, Ghaziabad 201002, India; [Sridhar, Balasubramanian] CSIR Indian Inst Chem Technol, Dept Analyt & Struct Chem, Hyderabad 500007, India in 2021.0, Cited 61.0. SDS of cas: 120-14-9. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

A highly regio- and stereoselective method was developed for the preparation of N-alkenylpyrazoles and chromenopyrazoles by the reaction of N-tosylhydrazones and salicyl N-tosylhydrazones with alkynes under neat conditions in the presence of La(OTf)(3). The present study was found to be efficient and convenient for direct access to N-alkenylpyrazoles and chromenopyrazoles through C-C, C-N, and C-O bond forming reactions. Structure assignment of N-alkenylpyrazole compound 5c was confirmed by X-ray analysis.

SDS of cas: 120-14-9. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Kurma, SH; Sridhar, B; Bhimapaka, CR 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