Category: 98-17-9

HPLC of Formula: C7H5F3O. In 2019 J MED CHEM published article about EXPRESSION; INHIBITOR; INFECTION; AGENTS; REPLICATION; METHYLATION; PREDICTION; RESERVOIRS; GENES; DRUGS in [Nguyen, William; Jarman, Kate E.; Sabroux, Helene Jousset; Sleebs, Brad E.] Walter & Eliza Hall Inst Med Res, Parkville, Vic 3052, Australia; [Nguyen, William; Jarman, Kate E.; Sabroux, Helene Jousset; Sleebs, Brad E.] Univ Melbourne, Dept Med Biol, Parkville, Vic 3052, Australia; [Jacobson, Jonathan; Harty, Leigh; Purcell, Damian F.] Univ Melbourne, Peter Doherty Inst Infect & Immun, Dept Microbiol & Immunol, Parkville, Vic 3000, Australia; [McMahon, James; Lewin, Sharon R.] Alfred Hlth, Dept Infect Dis, Melbourne, Vic 3004, Australia; [McMahon, James; Lewin, Sharon R.] Monash Univ, Melbourne, Vic 3004, Australia; [Lewin, Sharon R.] Univ Melbourne, Peter Doherty Inst Infect & Immun, Parkville, Vic 3000, Australia; [Lewin, Sharon R.] Royal Melbourne Hosp, Parkville, Vic 3000, Australia in 2019, Cited 49. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9.

The persistent reservoir of cells latently infected with human immunodeficiency virus (HIV)-integrated proviral DNA necessitates lifelong suppressive antiretroviral therapy (ART). Epigenetic targeted compounds have shown promise as potential latency-reversing agents; however, these drugs have undesirable toxicity and lack specificity for HIV. We utilized a novel HEK293-derived FlpIn dual-reporter cell line, which quantifies specific HIV provirus reactivation (LTR promoter) relative to nonspecific host cell gene expression (CMV promoter), to identify the 5-substituted 2-acylaminothiazole hit class. Here, we describe the optimization of the hit class, defining the functionality necessary for HIV gene activation and for improving in vitro metabolism and solubility. The optimized compounds displayed enhanced HIV gene expression in HEK293 and Jurkat 10.6 latency cellular models and increased unspliced HIV RNA in resting CD4+ T cells isolated from HIV-infected individuals on ART, demonstrating the potential of the 2-acylaminothiazole class as latency-reversing agents.

HPLC of Formula: C7H5F3O. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Nguyen, W; Jacobson, J; Jarman, KE; Sabroux, HJ; Harty, L; McMahon, J; Lewin, SR; Purcell, DF; Sleebs, BE 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

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

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

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

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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

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

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Nevesely, T; Daniliuc, CG; Gilmour, R or concate me.. Category: indole-building-block

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

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

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

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Lardy, SW; Luong, KC; Schmidt, VA or concate me.. Category: indole-building-block

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Recommanded Product: 98-17-9. I found the field of Pharmacology & Pharmacy very interesting. Saw the article Cinnamonitrile Adjuvants Restore Susceptibility to beta-Lactams against Methicillin-Resistant Staphylococcus aureus published in 2019, Reprint Addresses Mobashery, S (corresponding author), Univ Notre Dame, Dept Chem & Biochem, Notre Dame, IN 46556 USA.. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol.

beta-Lactams are used routinely to treat Staphylococcus aureus infections. However, the emergence of methicillin-resistant S. aureus (MRSA) renders them clinically precarious. We describe a class of cinnamonitrile adjuvants that restore the activity of oxacillin (a penicillin member of the beta-lactams) against MRSA. The lead adjuvants were tested against six important strains of MRSA, one vancomycin-intermediate S. aureus (VISA) strain, and one linezolid-resistant S. aureus strain. Five compounds out of 84 total compounds showed broad potentiation. At 8 mu M (E)-3-(5-(3,4-dichlorobenzy1)-2-(trifluoromethoxy)phenyl)-2-(methylsulfonyl)acrylonitrile (26) potentiated oxacillin with a >4000-fold reduction of its MIC (from 256 to 0.06 mg.L-1). This class of adjuvants holds promise for reversal of the resistance phenotype of MRSA.

Recommanded Product: 98-17-9. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Speri, E; Kim, C; De Benedetti, S; Qian, YY; Lastochkin, E; Fishovitz, J; Fisher, JF; Mobashery, 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

Yin, WY; Pan, XZ; Leng, WX; Chen, J; He, HF in [Yin, Weiyan; Pan, Xizhi; Leng, Wenxi] Wuhan Text Univ, Hubei Key Lab Biomass Fibers & Ecodyeing & Finish, Sch Chem & Chem Engn, Wuhan 430073, Hubei, Peoples R China; [Chen, Jian] Wuhan Univ Technol, Sch Chem Chem Engn & Lift Sci, Wuhan 430070, Hubei, Peoples R China; [He, Haifeng] Jiangxi Sci & Technol Normal Univ, Sch Chem & Chem Engn, Nanchang 330013, Jiangxi, Peoples R China published The highly efficient air oxidation of aryl and alkyl boronic acids by a microwave-assisted protocol under transition metal-free conditions in 2019, Cited 30. Recommanded Product: 98-17-9. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9.

Molecular oxygen is the most important green-oxidant due to its excellent properties. However, the effective utilization of molecular oxygen remains a major challenge in modern chemistry. Herein, we report the development a rapid, green and efficient microwave-assisted protocol for the air oxidation of boronic acids to phenols and alcohols under transition metal-free conditions. In the presence of KOH and DMSO, high yields of the expected phenols and alcohol were obtained with microwave-assistance, and a variety of functional groups were tolerated in this procedure. Notably, this transition metal-free method represents a breakthrough in both organic synthesis and green chemistry for the oxidative hydroxylation of boronic acids to phenols and alcohols.

Recommanded Product: 98-17-9. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Yin, WY; Pan, XZ; Leng, WX; Chen, J; He, HF 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 Discovery of Potent, Reversible, and Competitive Cruzain Inhibitors with Trypanocidal Activity: A Structure-Based Drug Design Approach WOS:000516665600059 published article about CHAGAS-DISEASE; CYSTEINE PROTEASE; LIGAND EFFICIENCY; DOCKING; LEADS; STRAINS in [de Souza, Mariana L.; Ferreira, Leonardo L. G.; Magalhaes, Luma G.; Krogh, Renata; Oliva, Glaucius; Andricopulo, Adriano D.] Univ Sao Paulo, Phys Inst Sao Carlos, Lab Med & Computat Chem, BR-13563120 Sao Carlos, SP, Brazil; [Rezende Junior, Celso de Oliveira; Espinoza Chavez, Rocio Marisol; Slafer, Brian W.; Dias, Luiz Carlos] Univ Estadual Campinas, Inst Chem, BR-13084971 Campinas, SP, Brazil; [Ferreira, Rafaela S.] Univ Fed Minas Gerais, Dept Biochem & Immunol, BR-31270901 Belo Horizonte, MG, Brazil; [Cruz, Fabio Cardoso] Univ Fed Sao Paulo, Dept Pharmacol, BR-04023062 Sao Paulo, SP, Brazil in 2020, Cited 38. Category: indole-building-block. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9

A virtual screening conducted with nearly 4 000 000 compounds from lead-like and fragment-like subsets enabled the identification of a small-molecule inhibitor (1) of the Trypanosoma cruzi cruzain enzyme, a validated drug target for Chagas disease. Subsequent comprehensive structure-based drug design and structure-activity relationship studies led to the discovery of carbamoyl imidazoles as potent, reversible, and competitive cruzain inhibitors. The most potent carbamoyl imidazole inhibitor (45) exhibited high affinity with a K-i value of 20 nM, presenting both in vitro and in vivo activity against T. cruzi. Furthermore, the most promising compounds reduced parasite burden in vivo and showed no toxicity at a dose of 100 mg/kg. These carbamoyl imidazoles are structurally attractive, nonpeptidic, and easy to prepare and synthetically modify. Finally, these results further advance our understanding of the noncovalent mode of inhibition of this pharmaceutically relevant enzyme, building strong foundations for drug discovery efforts.

Category: indole-building-block. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact de Souza, ML; Rezende , CD; Ferreira, RS; Chavez, RME; Ferreira, LLG; Slafer, BW; Magalhaes, LG; Krogh, R; Oliva, G; Cruz, FC; Dias, LC; Andricopulo, AD 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 Rhodium-Catalyzed ortho-Selective Carbene C-H Insertion of Unprotected Phenols Directed by a Transient Oxonium Ylide Intermediate WOS:000513082700030 published article about BOND FUNCTIONALIZATION; DIAZO-COMPOUNDS; N-TOSYLHYDRAZONES; ORTHO-ARYLATION; ALKENYLATION; ACTIVATION; ALKYLATION; LIGANDS; DIAZOESTERS; OLEFINS in [Guo, Rui-Ting; Zhang, Ya-Lin; Tian, Jun-Jie; Zhu, Ke-Yu; Wang, Xiao-Chen] Nankai Univ, Tianjin, Peoples R China in 2020, Cited 56. Category: indole-building-block. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9

ortho-Selective carbene C-H insertion of unprotected phenols is achieved with dimethyl diazomalonate under the catalysis of [Rh(COD)Cl](2). After the C-H insertion, subsequent cyclization and electrophilic addition of another carbene molecule affords tris-carboxylate-substituted 2-benzofuranones as the final reaction products. The enantioselective variant has been developed with the use of chiral diene ligands. Mechanistic experiments indicate that a transient oxonium ylide directing group might be responsible for the regiocontrol at the C-H activation step.

Category: indole-building-block. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Guo, RT; Zhang, YL; Tian, JJ; Zhu, KY; Wang, XC 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 Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article Regioselective Monobromination of Phenols with KBr and ZnAl-BrO3–Layered Double Hydroxides published in 2020. Computed Properties of C7H5F3O, Reprint Addresses Wang, LG; Hu, J (corresponding author), Zhejiang Univ Technol, Coll Chem Engn, Hangzhou 310004, Peoples R China.. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol

The regioselective mono-bromination of phenols has been successfully developed with KBr and ZnAl-BrO3–layered double hydroxides (abbreviated as ZnAl-BrO3–LDHs) as brominating reagents. The para site is much favorable and the ortho site takes the priority if para site is occupied. This reaction featured with excellent regioselectivity, cheap brominating reagents, mild reaction condition, high atom economy, broad substrate scope, and provided an efficient method to synthesize bromophenols.

Computed Properties of C7H5F3O. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Wang, LG; Feng, C; Zhang, Y; Hu, J 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 Discovery of Potent, Reversible, and Competitive Cruzain Inhibitors with Trypanocidal Activity: A Structure-Based Drug Design Approach WOS:000516665600059 published article about CHAGAS-DISEASE; CYSTEINE PROTEASE; LIGAND EFFICIENCY; DOCKING; LEADS; STRAINS in [de Souza, Mariana L.; Ferreira, Leonardo L. G.; Magalhaes, Luma G.; Krogh, Renata; Oliva, Glaucius; Andricopulo, Adriano D.] Univ Sao Paulo, Phys Inst Sao Carlos, Lab Med & Computat Chem, BR-13563120 Sao Carlos, SP, Brazil; [Rezende Junior, Celso de Oliveira; Espinoza Chavez, Rocio Marisol; Slafer, Brian W.; Dias, Luiz Carlos] Univ Estadual Campinas, Inst Chem, BR-13084971 Campinas, SP, Brazil; [Ferreira, Rafaela S.] Univ Fed Minas Gerais, Dept Biochem & Immunol, BR-31270901 Belo Horizonte, MG, Brazil; [Cruz, Fabio Cardoso] Univ Fed Sao Paulo, Dept Pharmacol, BR-04023062 Sao Paulo, SP, Brazil in 2020, Cited 38. Category: indole-building-block. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9

A virtual screening conducted with nearly 4 000 000 compounds from lead-like and fragment-like subsets enabled the identification of a small-molecule inhibitor (1) of the Trypanosoma cruzi cruzain enzyme, a validated drug target for Chagas disease. Subsequent comprehensive structure-based drug design and structure-activity relationship studies led to the discovery of carbamoyl imidazoles as potent, reversible, and competitive cruzain inhibitors. The most potent carbamoyl imidazole inhibitor (45) exhibited high affinity with a K-i value of 20 nM, presenting both in vitro and in vivo activity against T. cruzi. Furthermore, the most promising compounds reduced parasite burden in vivo and showed no toxicity at a dose of 100 mg/kg. These carbamoyl imidazoles are structurally attractive, nonpeptidic, and easy to prepare and synthetically modify. Finally, these results further advance our understanding of the noncovalent mode of inhibition of this pharmaceutically relevant enzyme, building strong foundations for drug discovery efforts.

Category: indole-building-block. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact de Souza, ML; Rezende , CD; Ferreira, RS; Chavez, RME; Ferreira, LLG; Slafer, BW; Magalhaes, LG; Krogh, R; Oliva, G; Cruz, FC; Dias, LC; Andricopulo, AD 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