Tag: 200-300

Wang, Juan; Liang, Boqiang; Chen, Yiling; Fuk-Woo Chan, Jasper; Yuan, Shuofeng; Ye, Hui; Nie, Linlin; Zhou, Jiao; Wu, Yi; Wu, Meixian; Huang, Lina S.; An, Jing; Warshel, Arieh; Yuen, Kwok-Yung; Ciechanover, Aaron; Huang, Ziwei; Xu, Yan published an article in 2021. The article was titled 《A new class of α-ketoamide derivatives with potent anticancer and anti-SARS-CoV-2 activities》, and you may find the article in European Journal of Medicinal Chemistry.Related Products of 7524-52-9 The information in the text is summarized as follows:

Inhibitors of the proteasome have been extensively studied for their applications in the treatment of human diseases such as hematol. malignancies, autoimmune disorders, and viral infections. Many of the proteasome inhibitors reported in the literature target the non-primed site of proteasome′s substrate binding pocket. In this study, we designed, synthesized and characterized a series of novel α-keto phenylamide derivatives aimed at both the primed and non-primed sites of the proteasome. In these derivatives, different substituted Ph groups at the head group targeting the primed site were incorporated in order to investigate their structure-activity relationship and optimize the potency of α-keto phenylamides. In addition, the biol. effects of modifications at the cap moiety, P1, P2 and P3 side chain positions were explored. Many derivatives displayed highly potent biol. activities in proteasome inhibition and anticancer activity against a panel of six cancer cell lines, which were further rationalized by mol. modeling analyses. Furthermore, a representative α-ketoamide derivative was tested and found to be active in inhibiting the cellular infection of SARS-CoV-2 which causes the COVID-19 pandemic. These results demonstrate that this new class of α-ketoamide derivatives are potent anticancer agents and provide exptl. evidence of the anti-SARS-CoV-2 effect by one of them, thus suggesting a possible new lead to develop antiviral therapeutics for COVID-19.H-Trp-OMe.HCl(cas: 7524-52-9Related Products of 7524-52-9) was used in this study.

H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.Related Products of 7524-52-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Sheng, Tao; Kong, Mengmeng; Wang, Yujie; Wu, HuiJun; Gu, Qin; Chuang, Anita Shyying; Li, Shengkun; Gao, Xuewen published their research in European Journal of Medicinal Chemistry in 2021. The article was titled 《Discovery and preliminary mechanism of 1-carbamoyl β-carbolines as new antifungal candidates》.Application of 7524-52-9 The article contains the following contents:

Various 1-substituted β-carbolines I (R1 = CH3, C6H5, 4-BrC6H4, etc.), II (R2 = C6H5, CONH2, CONHC6H5, etc.), III (R3 = Me, Ph, OH, etc.) and IV (R4 = Me, Ph, 2-pyridyl, etc.) were synthesized from com. inexpensive tryptophan and demonstrated significant in vitro antifungal activity against G. graminis. Significantly, compound II (R2 = CONH2) (EC50 = 0.45μM) with carboxamide at 1-position displayed the best efficacy and nearly 20 folds enhancement in antifungal potential compared to Silthiopham (EC50 = 8.95μM). Moreover, compounds 4,9-dihydro-3H-pyrido[3,4-b]indole-1-carboxamide, 9H-pyrido [3,4-b]indole-1-carboxamide, and II (R2 = CO2Me) exhibited excellent in vitro antifungal activities and in vivo protective and curative activities against B. cinerea and F. graminearum. Preliminary mechanism studies revealed that compound II (R2 = CONH2) caused reactive oxygen species accumulation, cell membrane destruction, and deregulation of histone acetylation. These findings indicated that 1-carbamoyl β-carbolines I, II, III and IV can be selected as a promising model for the discovery of novel and broad-spectrum fungicide candidates.H-Trp-OMe.HCl(cas: 7524-52-9Application of 7524-52-9) was used in this study.

H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.Application of 7524-52-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Scheiner, Matthias; Hoffmann, Matthias; He, Feng; Poeta, Eleonora; Chatonnet, Arnaud; Monti, Barbara; Maurice, Tangui; Decker, Michael published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Selective Pseudo-irreversible Butyrylcholinesterase Inhibitors Transferring Antioxidant Moieties to the Enzyme Show Pronounced Neuroprotective Efficacy In Vitro and In Vivo in an Alzheimer’s Disease Mouse Model》.Quality Control of N-Boc-1,6-Diaminohexane The article contains the following contents:

A series of multitarget-directed ligands (MTDLs) was designed by functionalizing a pseudo-irreversible butyrylcholinesterase (BChE) inhibitor. The obtained hybrids were investigated in vitro regarding their hBChE and hAChE inhibition, their enzyme kinetics, and their antioxidant physicochem. properties (DPPH, ORAC, metal chelating). In addition, in vitro assays were applied to investigate antioxidant effects using murine hippocampal HT22 cells and immunomodulatory effects on the murine microglial N9 cell line. The MTDLs retained their antioxidative properties compared to the parent antioxidant-moieties in vitro and the inhibition of hBChE was maintained in the submicromolar range. Representative compounds were tested in a pharmacol. Alzheimer’s disease (AD) mouse model and demonstrated very high efficacy at doses as low as 0.1 mg/kg. The most promising compound was also tested in BChE-/- mice and showed reduced efficacy. In vivo neuroprotection by BChE inhibition can be effectively enhanced by incorporation of structurally diverse antioxidant moieties. In the experimental materials used by the author, we found N-Boc-1,6-Diaminohexane(cas: 51857-17-1Quality Control of N-Boc-1,6-Diaminohexane)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) can be used as a linear hexyl spacer (C6-spacer) to synthesize biodegradable poly(disulfide amine)s for gene delivery, a multifunctional dendrimer for theranostics and so on.Quality Control of N-Boc-1,6-Diaminohexane

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2019,Bioorganic & Medicinal Chemistry included an article by Serrano, Julio F.; Lee, JuYeon; Daniel Curet, L.; Hagler, Lauren D.; Bonson, Sarah E.; Schuster, Emma J.; Zimmerman, Steven C.. Formula: C10H22N2O2. The article was titled 《Development of novel macrocyclic small molecules that target CTG trinucleotide repeats》. The information in the text is summarized as follows:

We describe the mol. design, synthesis, and investigation of a series of acridine-triaminotriazine macrocycles that selectively bind to CTG trinucleotide repeats in DNA with minimal nonspecific binding. The limited conformational flexibility enforces the stacking of the triaminotriazine and acridine units. Isothermal titration calorimetry studies and Job plot analyses revealed that the ligands bound to d(CTG) mismatched sites. The acridine and triaminotriazine units were shown to intramolecularly π-stack in aqueous solutions Compared to a noncyclic analog, the macrocycles showed an almost 10-fold lower cytotoxicity in HeLa cells and up to 4-fold higher transcription inhibition of d(CTG·CAG)74. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Formula: C10H22N2O2)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Formula: C10H22N2O2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2016,Staegemann, M. H.; Graefe, S.; Haag, R.; Wiehe, A. published 《A toolset of functionalized porphyrins with different linker strategies for application in bioconjugation》.Organic & Biomolecular Chemistry published the findings.Related Products of 51644-96-3 The information in the text is summarized as follows:

The reaction of amines with pentafluorophenyl-substituted A3B-porphyrins has been used to obtain different useful reactive groups for further functionalization and/or conjugation of these porphyrins to other substrates or materials. Porphyrins with alkenyl, alkynyl, amino, azido, epoxide, hydroxyl, and maleimido groups have thus been synthesized. For the first time such functionalized porphyrins have been conjugated to hyperbranched polyglycerol (hPG) as a biocompatible carrier system for photodynamic therapy (PDT) using the copper(I)-catalyzed 1,3-dipolar cycloaddition (CuAAC). The photocytotoxicity of selected porphyrins as well as of the porphyrin-hPG-conjugates has been assessed in cellular assays with human epidermoid carcinoma A-253 and squamous carcinoma CAL-27 cells. For several biomedical applications a release of the active drug and/or fluorescent dye is desired. Therefore, addnl., the synthesis of A3B-porphyrins with cleavable linker moieties is presented, namely disulfide, cleavable in a reductive environment, and acetal linkers whose cleavage is pH triggered. After reading the article, we found that the author used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Related Products of 51644-96-3)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Related Products of 51644-96-3

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Lyttle, Matthew H.; Hocker, Michael D.; Hui, Hon C.; Caldwell, Colby G.; Aaron, Decius T.; Engqvist-Goldstein, Asa; Flatgaard, Jeffrey E.; Bauer, Karin E. published an article on January 7 ,1994. The article was titled 《Isoenzyme-specific glutathione-S-transferase inhibitors: design and synthesis》, and you may find the article in Journal of Medicinal Chemistry.Application In Synthesis of H-Phg-OEt.HCl The information in the text is summarized as follows:

Glutathione-S-transferase (GST) isoenzyme-selective inhibitors H-Glu[Cys(R)-X-OH]-OH [I; R = (CH2)5Me, CH2Ph, CH2C6H4R1-4, R1 = Me, Cl, NO2, CMe3, OMe; X = Gly, β-Ala, (R)-phenylglycine] were designed by an empirically guided strategy. In the first phase, literature data were used to select C-terminal modifications which generated maximum variation in the catalytic efficiency (Vmax/Km) for I used as substrates with different rat GSTs. Also, on the basis of literature data, the sulfhydryl group was functionalized with a selection of alkyl and aryl groups to maximize potential isoenzyme specificity. Affinity chromatog. sorbents were prepared from I which showed isoenzyme selectivity for both rat tissue and recombinant human GST isoenzymes. Some I also showed selective inhibition of GST activity in catalysis of the reaction of 1-chloro-2,4-dinitrobenzene with glutathione (GSH). In the second phase, electronic effects were explored through synthesis of an isostructural series of S-benzyl GSH ligands with different substituents on the aromatic ring. GST isoenzyme specificity for these ligands, measured by binding to derivatized sorbents, varied substantially, with hydrophobic substituents favoring the human GST M1a isoenzyme and electroneg. moieties favoring GST P1. In the third phase, information obtained from testing both series of compounds was combined and used to prepare GSH analogs with chem. features responsible for isoenzyme specificity at both the C-terminus and the sulfur. This approach gave I [R = CH2C6H4Me-4, X = β-Ala; R = CH2C6H4Cl-4, X = (R)-phenylglycine], which showed improved potency while still maintaining selectivity in the inhibition of GSTs. A detailed discussion of the logic used in the selection of functional groups for maximum potency and selectivity is included. After reading the article, we found that the author used H-Phg-OEt.HCl(cas: 59410-82-1Application In Synthesis of H-Phg-OEt.HCl)

H-Phg-OEt.HCl(cas: 59410-82-1) belongs to esters. They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils.Application In Synthesis of H-Phg-OEt.HCl They perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Quality Control of H-Phg-OEt.HClOn March 31, 2003, Vicente, Virginie; Fruchier, Alain; Cristau, Henri-Jean published an article in Magnetic Resonance in Chemistry. The article was 《Determination of 31P, 31P coupling constants in cyclotriphosphazenes and their influence on 1H and 13C NMR spectra of phosphorus substituents》. The article mentions the following:

1H and 13C NMR spectra of sym. substituted cyclotriphenylosphazenes exhibit second-order effect0. The influence of the 31P,31P coupling constants between ring P atoms on these effects was studied. Some values of this coupling constant between P bearing identical substituents were measured using 13C satellites of the 31P signals or by introduction of a chiral substituent on the third P atom. In the experiment, the researchers used H-Phg-OEt.HCl(cas: 59410-82-1Quality Control of H-Phg-OEt.HCl)

H-Phg-OEt.HCl(cas: 59410-82-1) belongs to esters. They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils.Quality Control of H-Phg-OEt.HCl They perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

HPLC of Formula: 4033-88-9On March 30, 1999, Schroeder, Grzegorz; Leska, Boguslawa; Bartl, Franz; Rozalski, Bartosz; Brzezinski, Bogumil published an article in Journal of Molecular Structure. The article was 《Proton transfer reaction from some C-H acids to N-bases in polar aprotic solvents》. The article mentions the following:

The deprotonation reactions of di-Me (4-nitrophenyl)malonate and 4-bromophenyl-4-nitrophenylcyanomethane by tris[2-(2-methoxyethoxy)ethyl]amine, tributylamine and cryptand 222 were studied in polar aprotic solvents such as DMSO and acetonitrile by the kinetic, FT-IR and 1H NMR spectroscopic methods. The mechanisms of the proton transfer reactions are discussed. In addition to this study using Dimethyl 2-(4-nitrophenyl)malonate, there are many other studies that have used Dimethyl 2-(4-nitrophenyl)malonate(cas: 4033-88-9HPLC of Formula: 4033-88-9) was used in this study.

Dimethyl 2-(4-nitrophenyl)malonate(cas: 4033-88-9) belongs to esters.HPLC of Formula: 4033-88-9 They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils.Esters typically have a pleasant smell; those of low molecular weight are commonly used as fragrances and are found in essential oils and pheromones.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Name: Dimethyl 2-(4-nitrophenyl)malonateOn October 31, 1996 ,《Proton transfer reactions from dimethyl (4-nitrophenyl)malonate to N-bases in acetonitrile》 was published in Journal of Molecular Structure. The article was written by Schroeder, Grzegorz; Brzezinski, Bogumil; Jarczewski, Arnold; Grech, Eugeniusz; Milart, Piotr. The article contains the following contents:

Deprotonations of di-Me (4-nitrophenyl)malonate (C-acid) by 7-methyl-1,5,7-triazabicyclo[4.4.0]dec-5-ene (MTBD), 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD) and 1,8-bis(dimethylamino)naphthalene (DMAN) in acetonitrile were studied by kinetic as well as FTIR and 1H NMR spectroscopic methods. In the 1:1 mixture of C-acid with DMAN no proton transfer was found. The N-bases with guanidine-like character deprotonate C-acid in the acetonitrile solution quant. The mechanisms of proton transfer reactions are discussed.Dimethyl 2-(4-nitrophenyl)malonate(cas: 4033-88-9Name: Dimethyl 2-(4-nitrophenyl)malonate) was used in this study.

Dimethyl 2-(4-nitrophenyl)malonate(cas: 4033-88-9) belongs to esters. They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils.Name: Dimethyl 2-(4-nitrophenyl)malonate They perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Polyesters are important plastics, with monomers linked by ester moieties.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Recommanded Product: Dimethyl 2-(4-nitrophenyl)malonateOn May 18, 1998 ,《Solvent effects for proton transfer reaction from dimethyl (4-nitrophenyl)malonate to cis-1,2-bis(diethylaminomethyl)cyclohexane》 appeared in Journal of Molecular Structure. The author of the article were Schroeder, Grzegorz; Leska, Boguslawa; Brzezinski, Boguml. The article conveys some information:

The influence of polar aprotic solvents: DMSO, AN and HMPA on the kinetics of proton transfer reactions from dimethyl(4-nitrophenyl)malonate (C-acid) to cis-1,2-bis-(diethylaminomethyl)cyclohexane (DEAMCH) was studied. On the basis of the kinetic parameters obtained, the multistep mechanism of deprotonation processes and the influence of solvation on transition state were discussed. In the experiment, the researchers used Dimethyl 2-(4-nitrophenyl)malonate(cas: 4033-88-9Recommanded Product: Dimethyl 2-(4-nitrophenyl)malonate)

Dimethyl 2-(4-nitrophenyl)malonate(cas: 4033-88-9) belongs to esters. Esters are more polar than ethers but less polar than alcohols. They participate in hydrogen bonds as hydrogen-bond acceptors, but cannot act as hydrogen-bond donors, unlike their parent alcohols. Recommanded Product: Dimethyl 2-(4-nitrophenyl)malonate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics