Tag: 100-200

On January 7, 2019, Nakamura, Hidemitsu; Hirabayashi, Kei; Miyakawa, Takuya; Kikuzato, Ko; Hu, Wenqian; Xu, Yuqun; Jiang, Kai; Takahashi, Ikuo; Niiyama, Ruri; Dohmae, Naoshi; Tanokura, Masaru; Asami, Tadao published an article.Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole The title of the article was Triazole Ureas Covalently Bind to Strigolactone Receptor and Antagonize Strigolactone Responses. And the article contained the following:

Strigolactones, a class of plant hormones with multiple functions, mediate plant-plant and plant-microorganism communications in the rhizosphere. In this study, we developed potent strigolactone antagonists, which covalently bind to the strigolactone receptor D14, by preparing an array of triazole urea compounds Using yeast two-hybrid and rice-tillering assays, we identified a triazole urea compound KK094 as a potent inhibitor of strigolactone receptors. Liquid chromatog.-tandem mass spectrometry anal. and X-ray crystallog. revealed that KK094 was hydrolyzed by D14, and that a reaction product of this degradation covalently binds to the Ser residue of the catalytic triad of D14. Furthermore, we identified two triazole urea compounds KK052 and KK073, whose effects on D14-D53/D14-SLR1 complex formation were opposite due to the absence (KK052) or presence (KK073) of a trifluoromethyl group on their Ph ring. These results demonstrate that triazole urea compounds are potentially powerful tools for agricultural application and may be useful for the elucidation of the complicated mechanism underlying strigolactone perception. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole

The Article related to oryza tillering triazole urea strigolactone signaling, covalent antagonist, crystal structure, strigolactone, triazole urea, Agrochemical Bioregulators: Plant and other aspects.Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole

Referemce:
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

On September 1, 2015, Gehling, Victor S.; Vaswani, Rishi G.; Nasveschuk, Christopher G.; Duplessis, Martin; Iyer, Priyadarshini; Balasubramanian, Srividya; Zhao, Feng; Good, Andrew C.; Campbell, Robert; Lee, Christina; Dakin, Les A.; Cook, Andrew S.; Gagnon, Alexandre; Harmange, Jean-Christophe; Audia, James E.; Cummings, Richard T.; Normant, Emmanuel; Trojer, Patrick; Albrecht, Brian K. published an article.Quality Control of Methyl 2-methyl-1H-indole-3-carboxylate The title of the article was Discovery, design, and synthesis of indole-based EZH2 inhibitors. And the article contained the following:

The discovery and optimization of a series of small mol. EZH2 inhibitors is described. Starting from dimethylpyridone HTS hit, a series of indole-based EZH2 inhibitors were identified. Biochem. potency and microsomal stability were optimized during these studies and afforded compound (I). Compound I demonstrates nanomolar levels of biochem. potency (IC50 = 0.002 μM), cellular potency (EC50 = 0.080 μM), and afforded tumor regression when dosed (200 mpk SC BID) in an EZH2 dependent tumor xenograft model. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Quality Control of Methyl 2-methyl-1H-indole-3-carboxylate

The Article related to indole derivative preparation sar ezh2 inhibitor anticancer mao cell, ezh2, epigenetics, histone methyltransferase, prc2, pyridone, Pharmacology: Structure-Activity and other aspects.Quality Control of Methyl 2-methyl-1H-indole-3-carboxylate

Referemce:
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

On October 24, 1997, Bromidge, Steven M.; Duckworth, Malcolm; Forbes, Ian T.; Ham, Peter; King, Frank D.; Thewlis, Kevin M.; Blaney, Frank E.; Naylor, Christopher B.; Blackburn, Thomas P.; Kennett, Guy A.; Wood, Martyn D.; Clarke, Stephen E. published an article.Computed Properties of 52537-00-5 The title of the article was 6-Chloro-5-methyl-1-[[2-[(2-methyl-3- pyridyl)oxy]-5-pyridyl]carbamoyl]indoline (SB-242084): The First Selective and Brain Penetrant 5-HT2C Receptor Antagonist. And the article contained the following:

The synthesis and biol. activity of a number of substituted 1-(3-pyridylcarbamoyl)indolines is reported. These compounds are potent and selective 5-HT2C/2B receptor antagonists and illustrate the use of 5,6-disubstitution as a replacement for a fused 5-membered ring in this context. Unfortunately, some compounds were also found to be very potent inhibitors of a number of human cytochrome P 450 enzymes which precluded their development as potential anxiolytic agents. Elaboration of the left hand side pyridyl ring abolished the inhibitory activity, leading to bipyridylethers such as SB-242084 which is the first reported brain penetrant, 5-HT2C receptor antagonist with selectivity over both the 5-HT2A and 5-HT2B receptor subtypes. Furthermore, SB-242084 was found to exert marked anxiolytic-like responses in rat models, confirming that these responses are mediated by 5-HT2C receptor blockade. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Computed Properties of 52537-00-5

The Article related to pyridylcarbamoyl indoline preparation structure 5ht2c antagonist, sb242084 serotoninergic s2c receptor antagonist, Pharmacology: Structure-Activity and other aspects.Computed Properties of 52537-00-5

Referemce:
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

On October 8, 2015, Cleghorn, Laura A. T.; Albrecht, Sebastien; Stojanovski, Laste; Simeons, Frederick R. J.; Norval, Suzanne; Kime, Robert; Collie, Iain T.; De Rycker, Manu; Campbell, Lorna; Hallyburton, Irene; Frearson, Julie A.; Wyatt, Paul G.; Read, Kevin D.; Gilbert, Ian H. published an article.Safety of H-Idc-OH The title of the article was Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei. And the article contained the following:

There is an urgent need for new, brain penetrant small mols. that target the central nervous system second stage of human African trypanosomiasis (HAT). We report that a series of novel indoline-2-carboxamides have been identified as inhibitors of Trypanosoma brucei from screening of a focused protease library against Trypanosoma brucei brucei in culture. We describe the optimization and characterization of this series. Potent antiproliferative activity was observed The series demonstrated excellent pharmacokinetic properties, full cures in a stage 1 mouse model of HAT, and a partial cure in a stage 2 mouse model of HAT. Lack of tolerability prevented delivery of a fully curative regimen in the stage 2 mouse model and thus further progress of this series. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Safety of H-Idc-OH

The Article related to trypanosomicide indolinecarboxamide preparation structure activity brain penetrant trypanosomiasis, Pharmacology: Structure-Activity and other aspects.Safety of H-Idc-OH

Referemce:
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

On March 10, 2016, Pelz, Nicholas F.; Bian, Zhiguo; Zhao, Bin; Shaw, Subrata; Tarr, James C.; Belmar, Johannes; Gregg, Claire; Camper, DeMarco V.; Goodwin, Craig M.; Arnold, Allison L.; Sensintaffar, John L.; Friberg, Anders; Rossanese, Olivia W.; Lee, Taekyu; Olejniczak, Edward T.; Fesik, Stephen W. published an article.Recommanded Product: 79815-20-6 The title of the article was Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods. And the article contained the following:

Myeloid cell leukemia-1 (Mcl-1) is a member of the Bcl-2 family of proteins responsible for the regulation of programmed cell death. Amplification of Mcl-1 is a common genetic aberration in human cancer whose overexpression contributes to the evasion of apoptosis and is one of the major resistance mechanisms for many chemotherapies. Mcl-1 mediates its effects primarily through interactions with pro-apoptotic BH3 containing proteins that achieve high affinity for the target by utilizing four hydrophobic pockets in its binding groove. Here we describe the discovery of Mcl-1 inhibitors using fragment-based methods and structure-based design. These novel inhibitors exhibit low nanomolar binding affinities to Mcl-1 and >500-fold selectivity over Bcl-xL. X-ray structures of lead Mcl-1 inhibitors when complexed to Mcl-1 provided detailed information on how these small-mols. bind to the target and were used extensively to guide compound optimization. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Recommanded Product: 79815-20-6

The Article related to preparation indoleacylsulfonamide antitumor myeloid leukemia, crystal structure, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 79815-20-6

Referemce:
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

On December 15, 2006, Larsen, Scott D.; Hester, Matthew R.; Ruble, J. Craig; Kamilar, Gregg M.; Romero, Donna L.; Wakefield, Brian; Melchior, Earline P.; Sweeney, Michael T.; Marotti, Keith R. published an article.Computed Properties of 52537-00-5 The title of the article was Discovery and initial development of a novel class of antibacterials: Inhibitors of Staphylococcus aureus transcription/translation. And the article contained the following:

The novel bacterial transcription/translation (TT) inhibitor 1 was identified through a combination of high throughput screening and exploratory medicinal chem. Initial optimization of the anthranilic acid moiety and sulfonamide amine diversity was accomplished via 1- and two-dimensional solution phase libraries, resulting in an improvement in the MIC of the lead from 64 to 8 μg/mL (compound 4l). Subsequent modification of the central aromatic ring and further refinement of the sulfonamide amines required the development of a solid phase route on Wang resin. The resulting libraries generated a number of potent antibacterials with MICs of ≤1 μg/mL (e.g., 10b, 12, and 13). During the course of this work, it became apparent that the antibacterial activity of the series is not fully correlated with TT inhibition, suggesting that at least one addnl. mechanism of action is operative. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Computed Properties of 52537-00-5

The Article related to antibacterial staphylococcus aureus anthranilic acid derivative sar preparation, Pharmacology: Structure-Activity and other aspects.Computed Properties of 52537-00-5

Referemce:
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

Wang, Meng; Chen, Jun; Chen, Zongjia; Zhong, Changxu; Lu, Ping published an article in 2018, the title of the article was Enantioselective Desymmetrization of Cyclobutanones Enabled by Synergistic Palladium/Enamine Catalysis.Safety of H-Idc-OH And the article contains the following content:

The enantioselective intramol. α-arylation of cyclobutanones was established by combining palladium and enamine catalyst systems. Two different enantioselective control strategies were developed for cyclobutanone substrates bearing O- or N-tethered aryl bromides. Further synthetic applications are also reported. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Safety of H-Idc-OH

The Article related to cyclobutanone enantioselective desymmetrization palladium enamine catalyst, arylation, cyclobutanones, desymmetrization, palladium, synergistic catalysis, General Organic Chemistry: Synthetic Methods and other aspects.Safety of H-Idc-OH

Referemce:
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

On March 26, 2021, Shen, Meng-Lan; Wang, Pu-Sheng; Gong, Liu-Zhu published an article.Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole The title of the article was Counteranion-controlled regioselectivity in palladium-catalyzed allylic amination of dienyl allylic carbonates. And the article contained the following:

A regioselective Pd-catalyzed allylic amination reaction of dienyl allylic carbonates and aromatic amines has been developed by means of phosphoramidite-palladium catalysis. The regioselectivity could be altered by the counterion of the π-allylpalladium intermediate. As a result, either branched Z-dienyl allylic amines or linear conjugated allylic amines were generated in high levels of regioselectivity from the same substrates by tuning the reaction conditions. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole

The Article related to aryl amine dienyl allylic carbonate palladium catalyst regioselective amination, dienyl aryl amine preparation diastereoselective, General Organic Chemistry: Synthetic Methods and other aspects.Recommanded Product: 6-Chloro-2,3-dihydro-1H-indole

Referemce:
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

On July 14, 2020, Ouyang, Lu; Xia, YanPing; Wei, YiFei; Liao, Jianhua; Luo, Renshi published an article.Product Details of 79815-20-6 The title of the article was Highly Catalytic Enantioselective Reformatsky Reaction with Aldehydes and Ketones Using an Available Prolinol Ligand. And the article contained the following:

A highly Me2Zn-mediated catalytic enantioselective Reformatsky reaction of aldehydes and ketones with Et iodoacetate using a readily available prolinol ligand is reported. This reaction provides an efficient method for the construction of β-hydroxy esters in up to 98% yield and 95% enantiomeric excess (ee) value. A wide range of functional groups are tolerated and the practicality of this protocol is demonstrated by performing the reaction on a gram scale. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Product Details of 79815-20-6

The Article related to enantioselective reformatsky reaction aldehyde ketone iodoacetate prolinol ligand, hydroxy ester enantioselective synthesis, General Organic Chemistry: Synthetic Methods and other aspects.Product Details of 79815-20-6

Referemce:
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

On March 8, 2004, Blanc, Catherine; Agbossou-Niedercorn, Francine published an article.HPLC of Formula: 79815-20-6 The title of the article was Chiral aminophosphine-oxazoline auxiliaries applied to copper-catalyzed enantioselective 1,4-additions to enones. And the article contained the following:

A series of chiral aminophosphine-oxazoline auxiliaries has been prepared and applied in the copper-catalyzed 1,4-addition of diethylzinc to enones. The addition products are obtained quant. in up to 67% ee. The most efficient ligand of the series is based on L-indoline carboxylic acid and L-valinol. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).HPLC of Formula: 79815-20-6

The Article related to chiral aminophosphine oxazoline auxiliary preparation, copper catalyst enantioselective addition diethylzinc enone, General Organic Chemistry: Synthetic Methods and other aspects.HPLC of Formula: 79815-20-6

Referemce:
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