Tag: M.W=150-200

Recommanded Product: 98-17-9. In 2019 J THORAC IMAG published article about REPAIRED TETRALOGY; FALLOT; ECHOCARDIOGRAPHY; ADULTS; MANAGEMENT; SEVERITY in [Secchi, Francesco; Cannao, Paola M.; Di Leo, Giovanni; Sardanelli, Francesco] IRCCS Policlin San Donato, Radiol Unit, Milan, Italy; [Chessa, Massimo] IRCCS Policlin San Donato Milanese, Dept Pediat, Milan, Italy; [Chessa, Massimo] IRCCS Policlin San Donato Milanese, Adult Congenital Heart Ctr, Milan, Italy; [Monti, Caterina B.; Sardanelli, Francesco] Univ Milan, Dept Biomed Sci Hlth, Milan, Italy; [Ali, Marco] CDI, Unit Diagnost Imaging & Stereotact Radiosurg, Via St Bon 20, I-20147 Milan, Italy; [Petrini, Marcello] Guglielmo da Saliceto Hosp, Radiol Unit, Piacenza, Italy in 2019, Cited 26. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9.

Objective: The objective of this study was to compare the use of pulmonary regurgitation volume (PRV) or indexed PRV (PRVi) with that of pulmonary regurgitation fraction (PRF) in the assessment of patients with pulmonary regurgitation (PR) undergoing cardiac magnetic resonance (CMR) imaging. Materials and Methods: CMR of 176 patients with PR were retrospectively evaluated. Their right ventricular diastolic (end-diastolic volume index [EDVi]) and systolic (end-systolic volume index) volume indexes, stroke volume, and ejection fraction were obtained from cine CMR sequences, whereas phase-contrast flow sequences were analyzed to obtain PRV, PRVi, and PRF. Patients were divided into subgroups, according to underlying pathology and according to PR severity. Correlations between PRV or PRF and RV parameters were studied through Spearman rho, both in the main group and subgroups. Follow-up examinations were analyzed, and correlations between PRV or PRF from the first CMR examination and volume data from the second were calculated. Results: Tetralogy of Fallot was the main setting of PR (98/179). Overall, EDVi strongly correlates with PRV (rho=0.592, P<0.001) than with PRF (rho=0.522, P<0.001), and end-systolic volume index strongly correlates with PRV (rho=0.454, P<0.001) and PRF (rho=0.406, P <0.001). As regards subgroup analysis, in moderate or severe PR patients, EDVi strongly correlates (P=0.043) with PRV (rho=0.499, P<0.001) than with PRF (rho=0.317, P<0.001). Follow-up EDVi correlates with PRV (rho=0.450, P=0.031), but not with PRF. Conclusions: Especially when assessing moderate to severe PR, PRV and PRVi may be better indicators of right ventricular dysfunction than PRF. Moreover, PRV may be a predictor of worsening RV dilation. Recommanded Product: 98-17-9. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Secchi, F; Chessa, M; Petrini, M; Monti, CB; Ali, M; Cannao, PM; Di Leo, G; Sardanelli, F 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 Pugachev, MV; Pavelyev, RS; Nguyen, TNT; Gabbasova, RR; Bulatov, TM; Iksanova, AG; Aljondi, B; Bondar, OV; Grishaev, DY; Yamaleeva, ZR; Kataeva, ON; Nikishova, TV; Balakin, KV; Shtyrlin, YG in PERGAMON-ELSEVIER SCIENCE LTD published article about PHOSPHONIUM SALTS in [Pugachev, Mikhail, V; Pavelyev, Roman S.; Nguyen, Thang N. T.; Gabbasova, Raylya R.; Bulatov, Timur M.; Iksanova, Alfiya G.; Aljondi, Bashar; Bondar, Oksana, V; Grishaev, Denis Yu; Nikishova, Tatyana, V; Balakin, Konstantin, V; Shtyrlin, Yurii G.] Kazan Volga Reg Fed Univ, Kremlyovskaya 18, Kazan 420008, Russia; [Yamaleeva, Zilya R.; Kataeva, Olga N.] RAS, AE Arbuzov Inst Organ & Phys Chem, FRC Kazan Sci Ctr, Arbuzov Str 8, Kazan 420088, Russia in 2021.0, Cited 26.0. Recommanded Product: 3,4-Dimethoxybenzaldehyde. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

A new efficient approach to the synthesis of 6-alkenyl substituted pyridoxine derivatives has been developed. A series of 31 novel alkenyl pyridoxine derivatives, stilbene-based bioisosteric analogs of estradiol, were synthesized. In vitro cytotoxicity of the obtained compounds against MCF-7 (ER+) breast cancer tumor cells was studied using the MTT assay. The most active compounds with IC50, MCF-7 < 10 mu M were also tested for cytotoxicity in vitro against MDA-MB-231 (ER-) breast adenocarcinoma cells and conditionally normal human skin fibroblasts (HSF). The patterns of structure-antitumor activity relationships of the obtained compounds were analyzed. The most active compounds were found to contain a six-membered ketal ring, a methyl group in position 5, a 3,4-dimethoxystyryl fragment in positions 2 or 6 of the pyridoxine ring, and a trans-configuration of the double bond. Using the most active compound 5a as a representative cytotoxic agent, we have demonstrated that it has high specificity and antiproliferative activity against MCF-7 (ER+) tumor cells (IC50 < 5 mu M), and a higher therapeutic index compared to the reference compound raloxifene (48 versus 5.8). Compound 5a decreased the mitochondrial membrane potential and increased the level of reactive oxygen species in MCF-7 cells, but not MDA-MB-231 cells. Compound 5a did not affect the distribution of cell cycle phases and induced apoptosis in MCF-7 cells, but not MDA-MB-231. Unlike compound 5a, raloxifene decreased mitochondrial potential, increased the ROS level, and induced apoptosis in both MCF-7 and MDA-MB-231 cells, which indicated a lack of selectivity for cells with estrogen receptor expression. It was also shown that compound 5a reduced the level of ER alpha expression in cells to a lesser extent than raloxifene and, unlike the latter, did not activate the PI3K/Akt signaling pathway. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Pugachev, MV; Pavelyev, RS; Nguyen, TNT; Gabbasova, RR; Bulatov, TM; Iksanova, AG; Aljondi, B; Bondar, OV; Grishaev, DY; Yamaleeva, ZR; Kataeva, ON; Nikishova, TV; Balakin, KV; Shtyrlin, YG or concate me.. Recommanded Product: 3,4-Dimethoxybenzaldehyde

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: 3-(Trifluoromethyl)phenol. Recently I am researching about SELECTIVE-INHIBITION; GONDII; IDENTIFICATION; TRANSMISSION; ENCEPHALITIS; MECHANISM; DIAGNOSIS; INVASION; THERAPY; STRAINS, Saw an article supported by the Vyera Pharmaceuticals. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Janetka, JW; Hopper, AT; Yang, ZP; Barks, J; Dhason, MS; Wang, QL; Sibley, LD. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol

Calcium dependent protein kinase 1 (CDPK1) is an essential Ser/Thr kinase that controls invasion and egress by the protozoan parasite Toxoplasma gondii. The Gly gatekeeper of CDPK1 makes it exquisitely sensitive to inhibition by small molecule 1H-pyrazolo[3,4-d]pyrimidine-4-amine (PP) compounds that are bulky ATP mimetics. Here we rationally designed, synthesized, and tested a series of novel PP analogs that were evaluated for inhibition of CDPK1 enzyme activity in vitro and parasite growth in cell culture. Optimal substitution on the PP scaffold included 2-pyridyl ethers directed into the hydrophobic pocket and small carbocyclic rings accessing the ribose-binding pocket. Further optimization of the series led to identification of the lead compound 3a that displayed excellent potency, selectivity, safety profile, and efficacy in vivo. The results of these studies provide a foundation for further work to optimize CDPK1 inhibitors for the treatment of acute and chronic toxoplasmosis.

Name: 3-(Trifluoromethyl)phenol. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Janetka, JW; Hopper, AT; Yang, ZP; Barks, J; Dhason, MS; Wang, QL; Sibley, LD 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 Synthesis and Characterization of Magnetic Functionalized Ni and Cu Nano Catalysts and Their Application in Oxidation, Oxidative Coupling and Various Multi-Component Reactions WOS:000604191500004 published article about ONE-POT SYNTHESIS; RECYCLABLE CATALYST; EFFICIENT CATALYST; 5-SUBSTITUTED 1H-TETRAZOLES; SELECTIVE OXIDATION; HYDROGEN-PEROXIDE; IRON-OXIDE; NANOPARTICLES; SULFIDES; COMPLEX in [Hajjami, Maryam] Bu Ali Sina Univ, Dept Organ Chem, Fac Chem, Hamadan 6517838683, Hamadan, Iran; [Sheikhaei, Shiva; Gholamian, Fatemeh; Yousofvand, Zakieh] Ilam Univ, Fac Sci, Dept Chem, POB 69315516, Ilam, Iran in 2021.0, Cited 47.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9. Recommanded Product: 3,4-Dimethoxybenzaldehyde

Two magnetic nano catalysts of nickel and copper, Fe3O4@SiO2@DOP-BenPyr-M(II), (M=Ni and Cu) have been synthesized. These catalysts were applied as recoverable, efficient and new heterogeneous catalysts for the high yielding and room temperature one-pot procedure of selective oxidation of sulfides to sulfoxides and oxidative coupling of thiols to disulfides. In addition, the catalytic activity of Fe3O4@SiO2@DOP-BenPyr-Ni(II) was investigated as heterogeneous nanocatalyst for synthesis of 2,3-dihydroquinazolin-4(1H)-ones, 5-substituted 1H-tetrazoles and polyhydroquinolines. The synthesized catalysts were characterized by FT-IR, TGA, XRD, VSM, EDX, ICP and SEM techniques. These catalysts were recovered by an external magnet and reused several times without significant loss of catalytic efficiency. [GRAPHICS] .

Recommanded Product: 3,4-Dimethoxybenzaldehyde. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Hajjami, M; Sheikhaei, S; Gholamian, F; Yousofvand, Z 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-(Trifluoromethyl)phenol. In 2020 ANTIVIR RES published article about POLIOVIRUS; REPLICATION; PROTEIN; ATPASE; CLASSICS; MOTIF in [Manganaro, Roberto; Zonsics, Birgit; Lopez, Moira Lorenzo; Saporito, Fabiana; Ferla, Salvatore; Brancale, Andrea] Cardiff Univ, Sch Pharm & Pharmaceut Sci, King Edward VII Ave, Cardiff CF10 3NB, Wales; [Bauer, Lisa; Donselaar, Tim; Zwaagstra, Marleen; Strating, Jeroen R. P. M.; Hurdiss, Daniel L.; van Kuppeveld, Frank J. M.] Univ Utrecht, Fac Vet Med, Dept Infect Dis & Immunol, Virol Div, NL-3584 CL Utrecht, Netherlands; [Coutard, Bruno] UVE Aix Marseille Univ, Inserm 1207, IHU Mediterranee Infect, Unite Virus Emergents,IRD 190, Marseille, France; [Coutard, Bruno] Aix Marseille Univ, CNRS, AFMB UMR 7257, Marseille, France in 2020, Cited 24. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9.

Enteroviruses (EV) are a group of positive-strand RNA ( + RNA) viruses that include many important human pathogens (e.g. poliovirus, coxsackievirus, echovirus, numbered enteroviruses and rhinoviruses). Fluoxetine was identified in drug repurposing screens as potent inhibitor of enterovirus B and enterovirus D replication. In this paper we are reporting the synthesis and the antiviral effect of a series of fluoxetine analogues. The results obtained offer a preliminary insight into the structure-activity relationship of its chemical scaffold and confirm the importance of the chiral configuration. We identified a racemic fluoxetine analogue, 2b, which showed a similar antiviral activity compared to (S)-fluoxetine. Investigating the stereochemistry of 2b revealed that the Senantiomer exerts potent antiviral activity and increased the antiviral spectrum compared to the racemic mixture of 2b. In line with the observed antiviral effect, the Senantiomer displayed a dose-dependent shift in the melting temperature in thermal shift assays, indicative for direct binding to the recombinant 2C protein.

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Manganaro, R; Zonsics, B; Bauer, L; Lopez, ML; Donselaar, T; Zwaagstra, M; Saporito, F; Ferla, S; Strating, JRPM; Coutard, B; Hurdiss, DL; van Kuppeveld, FJM; Brancale, A or concate me.. Quality Control of 3-(Trifluoromethyl)phenol

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 Kinetically Controllable Pd-Catalyzed Decarboxylation Enabled [5+2] and [3+2] Cycloaddition toward Carbocycles Featuring Quaternary Carbons WOS:000643163800019 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. Application In Synthesis of 3,4-Dimethoxybenzaldehyde

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.. Application In Synthesis of 3,4-Dimethoxybenzaldehyde

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

COA of Formula: C9H7NO2. In 2019 J AGR FOOD CHEM published article about MICROBIAL-PRODUCTION; SALICYLATE BIOSYNTHESIS; PURIFICATION; ENZYME in [Choo, Hye Jeong; Ahn, Joong-Hoon] Konkuk Univ, Bio Mol Informat Ctr, Dept Biosci & Biotechnol, Seoul 05029, South Korea 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.

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.

COA of 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 Pharmacology & Pharmacy very interesting. Saw the article Hydroxyazole scaffold-based Plasmodium falciparum dihydroorotate dehydrogenase inhibitors: Synthesis, biological evaluation and X-ray structural studies published in 2019. Product Details of 98-17-9, Reprint Addresses Lolli, ML (corresponding author), Univ Turin, Dept Sci & Drug Technol, Via Pietro Giuria 9, I-10125 Turin, Italy.. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol

Plasmodium falciparum dihydroorotate dehydrogenase (PJDHODH) has been clinically validated as a target for antimalarial drug discovery, as a triazolopyrimidine class inhibitor (DSM265) is currently undergoing clinical development. Here, we have identified new hydroxyazole scaffold-based PJDHODH inhibitors belonging to two different chemical series. The first series was designed by a scaffold hopping strategy that exploits the use of hydroxylated azoles. Within this series, the hydroxythiadiazole 3 was identified as the best selective PJDHODH inhibitor (IC50 12.0 mu M). The second series was designed by modulating four different positions of the hydroxypyrazole scaffold. In particular, hydroxypyrazoles 7e and 7f were shown to be active in the low mu M range (IC50 2.8 and 5.3 mu M, respectively). All three compounds, 3, 7e and 7f showed clear selectivity over human DHODH (IC50> 200 mu M), low cytotoxicity, and retained micromolar activity in P. falciparum-infected erythrocytes. The crystallographic structures of PJDHODH in complex with compounds 3 and 7e proved their binding mode, supplying essential data for future optimization of these scaffolds. (C) 2018 Elsevier Masson SAS. All rights reserved.

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Pippione, AC; Sainas, S; Goyal, P; Fritzson, I; Cassiano, GC; Giraudo, A; Giorgis, M; Tavella, TA; Bagnati, R; Rolando, B; Caing-Carlsson, R; Costa, FTM; Andrade, CH; Al-Karadaghi, S; Boschi, D; Friemann, R; Lolli, ML or concate me.. Product Details of 98-17-9

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

SDS of cas: 120-14-9. Authors Duan, SZ; Deng, GG; Zi, YJ; Wu, XM; Tian, X; Liu, ZF; Li, MY; Zhang, HB; Yang, XD; Walsh, PJ in ROYAL SOC CHEMISTRY published article about in [Duan, Shengzu; Deng, Guogang; Zi, Yujin; Wu, Xiaomei; Tian, Xun; Liu, Zhengfen; Zhang, Hongbin; Yang, Xiaodong] Yunnan Univ, Sch Chem Sci & Technol, Yunnan Prov Ctr Res & Dev Nat Prod, Key Lab Med Chem Nat Resource,Minist Educ, Kunming 650091, Yunnan, Peoples R China; [Li, Minyan; Walsh, Patrick J.] Univ Penn, Dept Chem, Penn Merck Lab High Throughput Expt, Roy & Diana Vagelos Labs, 231 South 34th St, Philadelphia, PA 19104 USA 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

A unique enantioselective nickel-catalyzed vinylation of 2-azaallyl anions is advanced for the first time. This method affords diverse vinyl aryl methyl amines with high enantioselectivities, which are frequently occurring scaffolds in natural products and medications. This C-H functionalization method can also be extended to the synthesis of enantioenriched 1,3-diamine derivatives by employing suitably elaborated vinyl bromides. Key to the success of this process is the identification of a Ni/chiraphos catalyst system and a less reducing 2-azaallyl anion, all of which favor an anionic vinylation route over a background radical reaction. A telescoped gram scale synthesis and a product derivatization study confirmed the scalability and synthetic potential of this method.

About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Duan, SZ; Deng, GG; Zi, YJ; Wu, XM; Tian, X; Liu, ZF; Li, MY; Zhang, HB; Yang, XD; Walsh, PJ or concate me.. SDS of cas: 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

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. Safety of 4-Hydroxyquinolin-2(1H)-one

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.

Safety of 4-Hydroxyquinolin-2(1H)-one. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Elbastawesy, MAI; Aly, AA; Ramadan, M; Elshaier, YAMM; Youssif, BGM; Brown, AB; 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