Final Thoughts on Chemistry for 3-(Trifluoromethyl)phenol

Product Details of 98-17-9. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Kaitoh, K; Nakatsu, A; Mori, S; Kagechika, H; Hashimoto, Y; Fujii, S or concate me.

Product Details of 98-17-9. Kaitoh, K; Nakatsu, A; Mori, S; Kagechika, H; Hashimoto, Y; Fujii, S in [Kaitoh, Kazuma; Hashimoto, Yuichi; Fujii, Shinya] Univ Tokyo, Inst Quantitat Biosci, Bunkyo Ku, 1-1-1 Yayoi, Tokyo 1130032, Japan; [Nakatsu, Aki; Mori, Shuichi; Kagechika, Hiroyuki; Fujii, Shinya] Tokyo Med & Dent Univ, Inst Biomat & Bioengn, Chiyoda Ku, 2-3-10 Kanda Surugadai, Tokyo 1010062, Japan published Design, Synthesis and Biological Evaluation of Novel Nonsteroidal Progesterone Receptor Antagonists Based on Phenylamino-1,3,5-triazine Scaffold in 2019, Cited 33. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9.

We report here the development of phenylamino-1,3,5-triazine derivatives as novel nonsteroidal progesterone receptor (PR) antagonists. PR plays key roles in various physiological systems, including the female reproductive system, and PR antagonists are promising candidates for clinical treatment of multiple diseases. By using the phenylamino-1,3,5-triazine scaffold as a template structure, we designed and synthesized a series of 4-cyanophenylamino-1,3,5-triazine derivatives. The synthesized compounds exhibited PR antagonistic activity, and among them, compound 12n was the most potent (IC50 = 0.30 mu M); it also showed significant binding affinity to the PR ligand-binding domain. Docking simulation supported the design rationale of the compounds. Our results suggest that the phenylamino-1,3,5-triazine scaffold is a versatile template for development of nonsteroidal PR antagonists and that the developed compounds are promising lead compounds for further structural development of nonsteroidal PR antagonists.

Product Details of 98-17-9. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Kaitoh, K; Nakatsu, A; Mori, S; Kagechika, H; Hashimoto, Y; Fujii, 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

When did you first realize you had a special interest and talent in3-(Trifluoromethyl)phenol

Formula: C7H5F3O. Welcome to talk about 98-17-9, 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 send Email.

An article Synthesis and antiviral effect of novel fluoxetine analogues as enterovirus 2C inhibitors WOS:000540343900005 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. Formula: C7H5F3O

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.

Formula: C7H5F3O. Welcome to talk about 98-17-9, 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 send Email.

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

Chemistry Milestones Of C7H8O

Application In Synthesis of Benzyl Alcohol. About Benzyl Alcohol, If you have any questions, you can contact Adeel, M; Zhao, BJ; Mei, HG; Li, L; Zheng, SX or concate me.

An article Nanostructured thermosets involving epoxy and poly(ionic liquid)-Containing diblock copolymer WOS:000608415300002 published article about IONIC LIQUID; BLOCK-COPOLYMERS; RESIN; POLYMERIZATION; CRYSTALLIZATION; BLENDS; SEPARATION; CONVERSION; MEMBRANES; ANION in [Zheng, Sixun] Shanghai Jiao Tong Univ, Coll Chem & Chem Engn, Shanghai 200240, Peoples R China; Shanghai Jiao Tong Univ, State Key Lab Met Matrix Composites, Shanghai 200240, Peoples R China in 2021.0, Cited 50.0. Application In Synthesis of Benzyl Alcohol. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6

A novel poly(ionic liquid) (PIL)-containing diblock copolymer was synthesized via a sequential living/controlled polymerization approach. First, the ring-opening polymerization of epsilon-caprolactone (CL) was carried out to obtain a monohydroxyl-terminated PCL. The terminal hydroxyl group of the PCL chain was then exploited to react with carboxyl group of 2-(dodecylthiocarbonothioylthio)-2-methylpropanoic acid to obtain a trithiocarbonate-terminated PCL. Thereafter, such trithiocarbonate-terminated PCL was used to mediate the radical polymerization of tri-n-butyl-(4-vinylbenzyl) phosphoniumbis(trifluoromethane)sulfonamide (TBP+-TFSI-) to afford PIL diblock copolymers. Notably, the PIL diblock copolymers are capable of displaying self-assembly behavior in selective solvent (e.g., ethyl acetate). In the suspensions of ethyl acetate, the self-assembly generated the spherical micelles with the aggregates of P(TBP+-TFSI-) as the cores and with PCL blocks as the coronas. Such a self-assembly behavior was further employed to obtain epoxy thermoset with nanostructures. Owing to the introduction of fluorine-containing PIL diblock copolymer, the surface dewettability of the thermosets was significantly improved owing to the enrichment of P(TBP+-TFSI-) at the surface. The introduction of PIL microdomains in epoxy resulted that the dielectric constants of the materials were significantly enhanced. More importantly, the dielectric constants were temperature-dependent and can be further enhanced while the nanostructured thermosets were heated above the glass transition temperature of PIL blocks.

Application In Synthesis of Benzyl Alcohol. About Benzyl Alcohol, If you have any questions, you can contact Adeel, M; Zhao, BJ; Mei, HG; Li, L; Zheng, SX 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

Why Are Children Getting Addicted To 4-Methoxybenzaldehyde

Bye, fridends, I hope you can learn more about C8H8O2, If you have any questions, you can browse other blog as well. See you lster.. Quality Control of 4-Methoxybenzaldehyde

An article Novel Aminopyrazole Tagged Hydrazones as Anti-Tubercular Agents: Synthesis and Molecular Docking Studies WOS:000627232100004 published article about MYCOBACTERIUM-TUBERCULOSIS; BIOLOGICAL EVALUATION; INHIBITORS; DERIVATIVES; INHA; ANTIBACTERIAL; IDENTIFICATION; REDUCTASE; DESIGN; OPTIMIZATION in [Padmini, Thatavarthi; Kamal, Bigala Raj] Mewar Univ, Chittaurgarh, Rajasthan, India; [Bhikshapathi, Darna] Teegala Ram Reddy Coll Pharm, Hyderabad 500097, Telangana, India; [Suresh, Kandagatla] Vijaya Coll Pharm, Hyderabad 501511, Telangana, India; [Kulkarni, Ravindra] Bharati Vidyapeeths Poona Coll Pharm, Pune 411038, Maharashtra, India in 2021, Cited 44. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5. Quality Control of 4-Methoxybenzaldehyde

Background: Pyrazole derivatives have been reported to possess numerous pharmacological activities viz., anti-inflammatory, antipsychotic, etc. Our group has disclosed that pyrazole benzamides display potent antibacterial and anti-tubercular activities. Objective: Synthesis of new pyrazole acetamides which possess hydrazone group to be evaluated for antitubercular activity. Methods: The key intermediate 5-aminopyrazole was synthesized with the known procedure, which is then converted into chloroacetamide. This compound than resulted in hydrazine derivative and finally converted into aromatic hydrazones. All the compounds were screened for antitubercular activity. Result: All the synthesized compounds have been characterized by their spectral data obtained and subjected to anti-tubercular activity. Among all the twenty tested compounds, three compounds, 5a5, 5b5 and 5b7 have demonstrated MIC value of 3.12 mu g/mL against MTB H37Rv. Docking studies revealed important hydrogen bonding interactions with InhA. Conclusion: Three compounds 5a5, 5b5 and 5b7 were found to be most potent among the series of compounds. Docking studies of compounds explained the presence of hydrogen bonding and pp stacking interactions with InhA. Further synthesis of more such derivatives with optimized groups would produce compounds with more potent anti-tubercular activity.

Bye, fridends, I hope you can learn more about C8H8O2, If you have any questions, you can browse other blog as well. See you lster.. Quality Control of 4-Methoxybenzaldehyde

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

What I Wish Everyone Knew About C9H7NO2

Bye, fridends, I hope you can learn more about C9H7NO2, If you have any questions, you can browse other blog as well. See you lster.. Category: indole-building-block

In 2019 ORG LETT published article about ERIOSTEMON; SYNTHASE in [Coleman, Matthew A.; Burchill, Laura; Sumby, Christopher J.; George, Jonathan H.] Univ Adelaide, Dept Chem, Adelaide, SA 5005, Australia in 2019, Cited 12. 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 structure of furoerioaustralasine, a unique Australian alkaloid, has been revised based on a concise, biomimetic synthesis. The key step is a stereospecific, intramolecular ring opening of an epoxide to form a central dihydrofuran fused to a quinoline ring system.

Bye, fridends, I hope you can learn more about C9H7NO2, If you have any questions, you can browse other blog as well. See you lster.. 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

Some scientific research about 123-11-5

Recommanded Product: 4-Methoxybenzaldehyde. Bye, fridends, I hope you can learn more about C8H8O2, If you have any questions, you can browse other blog as well. See you lster.

An article An Efficient Regioselective Synthesis of 8-Formylhomoisoflavonoids with Neuroprotective Activity by Enhancing Autophagy WOS:000644478400047 published article about NATURALLY-OCCURRING HOMOISOFLAVONOIDS; BIOLOGICAL-ACTIVITIES; INHIBITION; CELLS in [Li, Jie; Yang, Fan; Zhang, Fang-Min] Zhejiang Univ City Coll, Sch Med, Dept Pharm, Hangzhou 310015, Peoples R China; [Zeng, Lin-Wei; Zhang, Fang-Min; Zhou, Chang-Xin; Gan, Li-She] Zhejiang Univ, Coll Pharmaceut Sci, Hangzhou 310058, Peoples R China; [Zhang, Fang-Min; Gan, Li-She] Wuyi Univ, Sch Biotechnol & Hlth Sci, Jiangmen 529020, Peoples R China in 2021, Cited 24. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5. Recommanded Product: 4-Methoxybenzaldehyde

6-Formylisoophiopogonone B (7a) and 8-formylophiopogonone B (7b), two natural products isolated from Ophiopogon japonicus, represent a subgroup of rare 6/8-formyl/methyl-homoisoflavonoid skeletons. Herein we report an efficient method for the synthesis of these formyl/methyl-homoisoflavonoids. The synthesized compounds were evaluated for their neuroprotective effects on the MPP(+)induced SH-SYSY cell injury model and showed marked activity. Exploration of the neuroprotective mechanisms of compound 7b led to an increased expression of autophagy marker LC3-II and down-regulation of autophagy substrate p62/SQSTM1. Molecular docking studies showed that 7b may prevent the inhibition of the classic PI3K-AKT-mTOR signaling pathway by interfering with the human HSP90AA1.

Recommanded Product: 4-Methoxybenzaldehyde. Bye, fridends, I hope you can learn more about C8H8O2, If you have any questions, you can browse other blog as well. See you lster.

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

Discover the magic of the 4′-Hydroxyacetophenone

Welcome to talk about 99-93-4, If you have any questions, you can contact Schena, T; Farrapeira, R; Erle, TRB; Krause, LC; von Muhlen, C; Caramao, EB or send Email.. Formula: C8H8O2

Formula: C8H8O2. Schena, T; Farrapeira, R; Erle, TRB; Krause, LC; von Muhlen, C; Caramao, EB in [Schena, Tiago; Caramao, Elina B.] Univ Fed Rio Grande do Sul UFRGS, Inst Quim, Porto Alegre, RS, Brazil; [Schena, Tiago; Caramao, Elina B.] Univ Fed Rio Grande do Sul, Inst Quim, Porto Alegre, RS, Brazil; [Farrapeira, Rafael; Erle, Thiago R. B.; Krause, Laiza C.; Caramao, Elina B.] Univ Tiradentes UNIT, Programa Posgrad Biotecnol Ind, Aracaju, SE, Brazil; [von Muhlen, Carin] UERJ, Dept Quim, Rezende, RJ, Brazil; [Krause, Laiza C.; Caramao, Elina B.] Univ Fed Bahia, INCTE&A, Salvador, BA, Brazil published Fast two-dimensional gas chromatography applied in the characterization of bio-oil from the pyrolysis of coconut fibers in 2019.0, Cited 31.0. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4.

The goal of this paper is the evaluation of fast two-dimensional gas chromatography applied to bio-oil samples. Bio-oils are complex matrixes that usually are analyzed by conventional gas chromatography, involving long columns, long time of analysis due to slow heating rates, and consequently, high cost associated to time consumed. Fast gas chromatography techniques are based on the use of narrow capillary columns that allow the achievement high-speed separations for complex samples, maintaining excellent resolution. Firstly, the two-dimensional gas chromatography method was optimized varying the heating rate (10, 15 and 20 degrees C min(-1)) and achieving the optimal separation at 15 degrees C min(-1). This method allies a good separation of bio-oil constituents with shorter time analysis. The developed method and the traditional conventional two-dimensional gas chromatography method (used in previous studies) were applied in the analysis of a mixture of 30 standard compounds. Despite coelutions of short retention time peaks (compounds with very similar physical-chemical properties), the fast two-dimensional gas chromatography method showed an increase in chromatographic signal and a noise reduction. Good results were also obtained in the real bio-oil sample. Fast two-dimensional gas chromatography maintained all the chromatographic information from conventional two-dimensional gas chromatography, reducing drastically the total time of analysis.

Welcome to talk about 99-93-4, If you have any questions, you can contact Schena, T; Farrapeira, R; Erle, TRB; Krause, LC; von Muhlen, C; Caramao, EB or send Email.. Formula: C8H8O2

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

Let`s talk about compound :3-(Trifluoromethyl)phenol

Name: 3-(Trifluoromethyl)phenol. Welcome to talk about 98-17-9, If you have any questions, you can contact Manfrin, A; Hanggli, A; van den Wildenberg, J; McNeill, K or send Email.

Authors Manfrin, A; Hanggli, A; van den Wildenberg, J; McNeill, K in AMER CHEMICAL SOC published article about MECHANISTIC ORGANIC-PHOTOCHEMISTRY; TFM; PHARMACEUTICALS; FLUORINE; WATER; PHOTOHYDROLYSIS; ENVIRONMENT; REACTIVITY; DRUGS; ACID in [Manfrin, Alessandro; Haenggli, Aline; van den Wildenberg, Jeroen; McNeill, Kristopher] Swiss Fed Inst Technol, Inst Biogeochem & Pollutant Dynam, CH-8092 Zurich, Switzerland in 2020, Cited 45. Name: 3-(Trifluoromethyl)phenol. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9

The chemical class of benzotrifluoride derivatives is widely used in active ingredients of various commercial products, such as pharmaceuticals, pesticides, herbicides, and crop protection agents. Past studies have shown that some benzotrifluorides are not stable under UV irradiation in water and convert into benzoic acids due to C-F bond hydrolysis. It was also observed, but never systematically studied, that the ring substituents play an important role on the direct photochemical reactivity of the CF3 moiety. In the present work, we explore the structure-reactivity relationship between ring substituent and direct photodefluorination for 16 different substituents, by determining fluoride production rates, quantum yields, and half-lives, and found that strong electron-donating groups enhance the reactivity toward hydrolysis. In addition, flufenamic acid, travoprost, dutasteride, cyflumetofen, flutoanil, and teriflunomide were also examined, finding that their direct photochemical reactivity could be qualitatively predicted based on their ring substituents. We provide here a tool to evaluate the environmental persistence of benzotrifluoride contaminants, as well as to design more photodegradable new active ingredients.

Name: 3-(Trifluoromethyl)phenol. Welcome to talk about 98-17-9, If you have any questions, you can contact Manfrin, A; Hanggli, A; van den Wildenberg, J; McNeill, K or send Email.

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

How did you first get involved in researching 3,4-Dimethoxybenzaldehyde

Quality Control of 3,4-Dimethoxybenzaldehyde. Bye, fridends, I hope you can learn more about C9H10O3, If you have any questions, you can browse other blog as well. See you lster.

Quality Control of 3,4-Dimethoxybenzaldehyde. Authors Sepehrmansourie, H; Zarei, M; Zolfigol, MA; Babaee, S; Rostamnia, S in NATURE RESEARCH published article about in [Sepehrmansourie, Hassan; Zarei, Mahmoud; Zolfigol, Mohammad Ali; Babaee, Saeed] Bu Ali Sina Univ, Fac Chem, Dept Organ Chem, Hamadan 6517838683, Hamadan, Iran; [Rostamnia, Sadegh] Iran Univ Sci & Technol IUST, Dept Chem, Organ & Nano Grp ONG, POB 16846-13114, Tehran, Iran; [Rostamnia, Sadegh] Univ Maragheh, Fac Sci, Dept Chem, Organ & Nano Grp ONG, POB 55181-83111, Maragheh, Iran in 2021.0, Cited 66.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

Herein, a new magnetic metal-organic frameworks based on Fe3O4 (NMMOFs) with porous and high surface area materials were synthesized. Then, NMMOFs were characterized by FT-IR, XRD, SEM, elemental mapping, energy dispersive X-ray (EDS), TG, DTG, VSM, and N-2 adsorption-desorption isotherms (BET). Fe3O4@Co(BDC)-NH2 as a magnetic porous catalyst was applied for synthesis of novel fused pyridines and 1,4-dihydropyridines with pyrazole and pyrimidine moieties as suitable drug candidates under ultrasonic irradiation. The significant advantages of the presented methodology are mild, facile workup, high yields, short reaction times, high thermal stability, and reusability of the described NMMOFs catalyst.

Quality Control of 3,4-Dimethoxybenzaldehyde. Bye, fridends, I hope you can learn more about C9H10O3, If you have any questions, you can browse other blog as well. See you lster.

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

Top Picks: new discover of 86-95-3

Category: indole-building-block. Bye, fridends, I hope you can learn more about C9H7NO2, If you have any questions, you can browse other blog as well. See you lster.

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

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.

Category: indole-building-block. Bye, fridends, I hope you can learn more about C9H7NO2, If you have any questions, you can browse other blog as well. See you lster.

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