Tag: M.W=150-200

Recommanded Product: 86-95-3. 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.

Recommanded Product: 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.

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 MOLECULES 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. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3. Category: indole-building-block

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.

Category: indole-building-block. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Ryzhkov, FV; Ryzhkova, YE; Elinson, MN; Vorobyev, SV; Fakhrutdinov, AN; Vereshchagin, AN; Egorov, MP 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

Marjani, AP; Khalafy, J; Farajollahi, A in [Marjani, Ahmad Poursattar; Khalafy, Jabbar; Farajollahi, Ayda] Urmia Univ, Dept Organ Chem, Fac Chem, Orumiyeh, Iran published Synthesis of Ethyl 2-Amino-4-benzoyl-5-oxo-5,6-dihydro-4H-pyrano[3,2-c]quinoline-3-carboxylates by a One-pot, Three-Component Reaction in the Presence of TPAB in 2019, Cited 41. 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.

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.

Application In Synthesis 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

In 2019 SYNOPEN published article about DIRECT N-ALKYLATION; O-ALKYLATION; REDUCTIVE AMINATION; ARYL ETHERS; EFFICIENT SYNTHESIS; AROMATIC-AMINES; ALCOHOLS; PHENOLS; ANILINES; DERIVATIVES in [Jagtap, Sangeeta V.] Baburaoji Gholap Coll, Dept Chem, Pune 411027, Maharashtra, India; Savitribai Phule Pune Univ, Pune, Maharashtra, India in 2019, Cited 115. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9. Computed Properties of C7H5F3O

A simple and efficient protocol for base-mediated selective synthesis of 2-(arylamino)ethanols from primary aromatic amines and 2-aryloxyethanols from phenols, promoted by K (2) CO (3) has been achieved under mild conditions. Even in presence of excess alkyl halide, selective mono-N-alkylation has been achieved. Tolerance of a variety of functional groups is demonstrated by 15 examples of selective N-alkylation of aromatic amines and 19 examples of O-alkylation of phenols. The efficacy of the protocol is demonstrated by the formal synthesis of Ticlopidine (-(R)) , Vildagliptin (R) , Quetiapine (R) , and Gemfibrozil (R).

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Sonawane, RB; Sonawane, SR; Rasal, NK; Jagtap, SV or concate me.. Computed Properties of C7H5F3O

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: C7H5F3O. Authors Mollasalehi, N; Francois-Moutal, L; Scott, DD; Tello, JA; Williams, H; Mahoney, B; Carlson, JM; Dong, Y; Li, XL; Miranda, VG; Gokhale, V; Wang, W; Barmada, SJ; Khanna, M in AMER CHEMICAL SOC published article about in [Mollasalehi, Niloufar; Francois-Moutal, Liberty; Scott, David D.; Tello, Judith A.; Williams, Haley; Carlson, Jacob M.; Miranda, Victor G.; Khanna, May] Univ Arizona, Coll Med, Dept Pharmacol, Tucson, AZ 85724 USA; [Mollasalehi, Niloufar; Francois-Moutal, Liberty; Scott, David D.; Tello, Judith A.; Williams, Haley; Carlson, Jacob M.; Miranda, Victor G.; Khanna, May] Ctr Innovat Brain Sci, Tucson, AZ 85721 USA; [Mollasalehi, Niloufar] Univ Arizona, Dept Chem & Biochem, Tucson, AZ 85721 USA; [Mahoney, Brendan] Univ Calif Los Angeles UCLA, Dept Chem & Biochem, Los Angeles, CA 90095 USA; [Dong, Yue; Wang, Wei] Univ Arizona, Coll Pharm, Arizona Ctr Drug Discovery, Tucson, AZ 85721 USA; [Dong, Yue; Wang, Wei] Univ Arizona, Coll Pharm, Pharmacol & Toxicol Dept, Tucson, AZ 85721 USA; [Li, Xingli; Barmada, Sami J.] Univ Michigan Hlth Syst, Dept Neurol, Ann Arbor, MI 48109 USA; [Gokhale, Vijay] Univ Arizona, Bio5 Inst, Tucson, AZ 85721 USA in 2020, Cited 23. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9

In this study, we targeted the N-terminal domain (NTD) of transactive response (TAR) DNA binding protein (TDP-43), which is implicated in several neurodegenerative diseases. In silico docking of 50K compounds to the NTD domain of TDP-43 identified a small molecule (nTRD22) that is bound to the N-terminal domain. Interestingly, nTRD22 caused allosteric modulation of the RNA binding domain (RRM) of TDP-43, resulting in decreased binding to RNA in vitro. Moreover, incubation of primary motor neurons with nTRD22 induced a reduction of TDP-43 protein levels, similar to TDP-43 RNA binding-deficient mutants and supporting a disruption of TDP43 binding to RNA. Finally, nTRD22 mitigated motor impairment in a Drosophila model of amyotrophic lateral sclerosis. Our findings provide an exciting way of allosteric modulation of the RNA-binding region of TDP-43 through the N-terminal domain.

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Mollasalehi, N; Francois-Moutal, L; Scott, DD; Tello, JA; Williams, H; Mahoney, B; Carlson, JM; Dong, Y; Li, XL; Miranda, VG; Gokhale, V; Wang, W; Barmada, SJ; Khanna, M or concate me.. Formula: C7H5F3O

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

Recommanded Product: 120-14-9. Authors Kumari, M; Tahlan, S; Narasimhan, B; Ramasamy, K; Lim, SM; Shah, SAA; Mani, V; Kakkar, S in BMC published article about in [Kumari, Mukesh; Tahlan, Sumit; Narasimhan, Balasubramanian; Kakkar, Saloni] Maharshi Dayanand Univ, Fac Pharmaceut Sci, Rohtak 124001, Haryana, India; [Ramasamy, Kalavathy; Lim, Siong Meng; Shah, Syed Adnan Ali] Univ Teknol MARA UiTM, Fac Pharm, Bandar Puncak Alam 42300, Selangor Darul, Malaysia; [Ramasamy, Kalavathy; Lim, Siong Meng] Univ Teknol MARA UiTM, Collaborat Drug Discovery Res CDDR Grp, Pharmaceut Life Sci Community Res, Shah Alam 40450, Selangor Darul, Malaysia; [Shah, Syed Adnan Ali] Univ Teknol MARA UiTM, Atta Ur Rahman Inst Nat Prod Discovery AuRIns, Puncak Alam Campus, Bandar Puncak Alam 42300, Selangor Darul, Malaysia; [Mani, Vasudevan] Qassim Univ, Dept Pharmacol & Toxicol, Coll Pharm, Buraydah 51452, Saudi Arabia in 2021.0, Cited 27.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

Background Triazole is an important heterocyclic moiety that occupies a unique position in heterocyclic chemistry, due to its large number of biological activities. It exists in two isomeric forms i.e. 1,2,4-triazole and 1,2,3-triazole and is used as core molecule for the design and synthesis of many medicinal compounds. 1,2,4-Triazole possess broad spectrum of therapeutically interesting drug candidates such as analgesic, antiseptic, antimicrobial, antioxidant, anti-urease, anti-inflammatory, diuretics, anticancer, anticonvulsant, antidiabetic and antimigraine agents. Methods The structures of all synthesized compounds were characterized by physicochemical properties and spectral means (IR and NMR). The synthesized compounds were evaluated for their in vitro antimicrobial activity against Gram-positive (B. subtilis), Gram-negative (P. aeruginosa and E. coli) bacterial and fungal (C. albicans and A. niger) strains by tube dilution method using ciprofloxacin, amoxicillin and fluconazole as standards. In-vitro antioxidant and anti-urease screening was done by DPPH assay and indophenol method, respectively. The in-vitro anticancer evaluation was carried out against MCF-7 and HCT116 cancer cell lines using 5-FU as standards. Results, discussion and conclusion The biological screening results reveal that the compounds T-5 (MICBS, EC = 24.7 mu M, MICPA, (CA) = 12.3 mu M) and T-17 (MICAN = 27.1 mu M) exhibited potent antimicrobial activity as comparable to standards ciprofloxacin, amoxicillin (MICCipro = 18.1 mu M, MICAmo = 17.1 mu M) and fluconazole (MICFlu = 20.4 mu M), respectively. The antioxidant evaluation showed that compounds T-2 (IC50 = 34.83 mu g/ml) and T-3 (IC50 = 34.38 mu g/ml) showed significant antioxidant activity and comparable to ascorbic acid (IC50 = 35.44 mu g/ml). Compounds T-3 (IC50 = 54.01 mu g/ml) was the most potent urease inhibitor amongst the synthesized compounds and compared to standard thiourea (IC50 = 54.25 mu g/ml). The most potent anticancer activity was shown by compounds T-2 (IC50 = 3.84 mu M) and T-7 (IC50 = 3.25 mu M) against HCT116 cell lines as compared to standard 5-FU (IC50 = 25.36 mu M).

About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Kumari, M; Tahlan, S; Narasimhan, B; Ramasamy, K; Lim, SM; Shah, SAA; Mani, V; Kakkar, S or concate me.. Recommanded Product: 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

Category: indole-building-block. 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.

Category: indole-building-block. 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

SDS of cas: 120-14-9. In 2021 RSC ADV published article about ONE-POT; MAGNETIC NANOPARTICLES; CLAISEN REARRANGEMENT; DERIVATIVES; EFFICIENT; GLYCALS; DRUGS; DECONTAMINATION; HETEROCYCLES; ANTICANCER in [Torabi, Morteza; Yarie, Meysam; Zolfigol, Mohammad Ali] Buali Sina Univ, Fac Chem, Dept Organ Chem, Hamadan 6517838683, Hamadan, Iran; [Rouhani, Shamila; Msagati, Titus A. M.] Univ South Africa, Coll Sci Engn & Technol, Inst Nanotechnol & Water Sustainabil iNanoWS, ZA-1709 Johannesburg, South Africa; [Azizi, Shohreh; Maaza, Malik] Univ South Africa, Coll Grad Studies, UNESCO UNISA Africa Chair Nanosci & Nanotech, POB 392, Pretoria, South Africa; [Azizi, Shohreh] iThemba LABS Natl Res Fdn, Nanosci African Network NANOAFNET, 1 Old Faure Rd,POB 722, ZA-7129 Western Cape, South Africa; [Olomola, Temitope O.] Obafemi Awolowo Univ, Dept Chem, Ife 220005, Nigeria; [Msagati, Titus A. M.] Nelson Mandela African Inst Sci & Technol, Sch Life Sci & Bioengn, POB 447, Arusha, Tanzania in 2021, Cited 96. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9.

In the present study, we reported the synthesis of a novel quinoline-based dendrimer-like ionic liquid. After characterization of the mentioned ionic liquid with suitable techniques such as Fourier transform infrared spectroscopy (FT-IR), energy dispersive X-ray spectroscopy (EDX), elemental mapping, thermogravimetric analysis (TGA) and derivative thermogravimetry (DTG), its catalytic performance was investigated in the synthesis of new pyridines with sulfonamide moiety via a cooperative vinylogous anomeric-based oxidation mechanism under mild reaction conditions. All target molecules were achieved in short reaction times and high yields.

SDS of cas: 120-14-9. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Torabi, M; Yarie, M; Zolfigol, MA; Rouhani, S; Azizi, S; Olomola, TO; Maaza, M; Msagati, TAM 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

Quality Control of 3,4-Dimethoxybenzaldehyde. I found the field of Chemistry very interesting. Saw the article BCl3 Catalyzed, Solvent Free Protocol for the Synthesis of Dihydropyrano[3,2-b] Chromenediones published in 2021, Reprint Addresses Mathapati, SR (corresponding author), Shri Madhavrao Patil Mahavidyalaya, Dept Chem, Murum 413605, India.; Mathapati, SR (corresponding author), Dr BAM Univ, Aurangabad, Maharashtra, India.. The CAS is 120-14-9. Through research, I have a further understanding and discovery of 3,4-Dimethoxybenzaldehyde.

Solvent free synthesis of dihydropyrano[3,2-b]chromenediones was formulated via multicomponent reactions of kojic acid, dimedone and several substituted aromatic aldehydes catalyzed with BCl3. Reactions progressed efficiently and the corresponding heterocyclic products were obtained in good to high yields within short period. The developed protocol is one of the better and efficient alternative methods for the synthesis of dihydropyrano[3,2-b]chromenediones. The simple reaction procedure, easy separation of products, radially available catalyst are certain benefits of this reported protocol.

Quality Control of 3,4-Dimethoxybenzaldehyde. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Suryawanshi, VB; Momin, KI; Dawle, JK; Mathapati, SR 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 Aly, AA; Ishak, E; Shwaky, AM; Mohamed, AH in SPRINGER WIEN published article about DERIVATIVES; INHIBITORS; FUROQUINOLINE; ALKALOIDS; MODEL in [Aly, Ashraf A.; Mohamed, Asmaa H.] Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt; [Ishak, Esam] Al Azhar Univ, Fac Sci, Dept Chem, Assiut, Egypt; [Ishak, Esam] Jouf Univ, Coll Sci & Arts, Dept Chem, Alquurrayate, Saudi Arabia; [Shwaky, Ahmed M.] Umm Al Qura Univ, STU, Mecca, Saudi Arabia in 2020, Cited 31. HPLC of Formula: C9H7NO2. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3

Quinoline-2,4-diones reacted with 2-[bis(methylthio)methylene]malononitrile in DMF/Et3N to produce 3-(methylthio)-4-oxo-4,5-dihydrofuro[3,2-c]quinolone-2-carbonitriles and 3-(methylthio)-4-oxo-4,5-dihydrofuro[3,2-c]quinolone-2-carboxamides in state of 2-imino-substituted 4-(methylthio)-5,6-dihydro-2H-pyrano[3,2-c]quinolone-3-carbonitriles. The structures of all new products were proved using NMR, IR, and mass spectral data. The possible mechanism for the reaction is also discussed. Graphic abstract

HPLC of Formula: C9H7NO2. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Aly, AA; Ishak, E; Shwaky, AM; Mohamed, AH 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