Category: 7524-52-9

Quality Control of H-Trp-OMe.HCl. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about A new class of α-ketoamide derivatives with potent anticancer and anti-SARS-CoV-2 activities. Author is 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.

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.

Although many compounds look similar to this compound(7524-52-9)Quality Control of H-Trp-OMe.HCl, numerous studies have shown that this compound(SMILES:N[C@@H](CC1=CNC2=CC=CC=C12)C(OC)=O.[H]Cl), has unique advantages. If you want to know more about similar compounds, you can read my other articles.

Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Lu, Meng-Chen; Zhang, Xian; Wu, Feng; Tan, Shi-Jie; Zhao, Jing; You, Qi-Dong; Jiang, Zheng-Yu published an article about the compound: H-Trp-OMe.HCl( cas:7524-52-9,SMILESS:N[C@@H](CC1=CNC2=CC=CC=C12)C(OC)=O.[H]Cl ).Safety of H-Trp-OMe.HCl. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:7524-52-9) through the article.

The transcription factor Nrf2 is a key regulator of cytoprotective system, and enhancing Nrf2 activity can protect cells from various insults and threats. Directly disrupting Keap1-Nrf2 protein-protein interactions has been regarded as a promising way to activate Nrf2. We reported here the first identification of amino acids as preferred substituents to design potent Keap1-Nrf2 inhibitors. Comprehensive structure-activity anal. identified Pro as a preferred substituent, obtaining a potent inhibitor 35 with an IC50 of 43 nM in the competitive fluoresce polarization (FP) assay and a Kd value of 53.7 nM for Keap1 protein in the isothermal titration calorimetry (ITC) assay. The Pro analog 35 exhibited tight and prolonged Keap1 binding in vitro and in cells, and treatment with 35 activated Nrf2-regulated cytoprotective response and antagonized acetaminophen-induced liver injury both in cellular and in vivo models. This work not only provides a useful tool to further explore the therapeutic potential of Keap1-Nrf2 inhibition but also enriches the diversity of chem. structures suitable for the Keap1-Nrf2 interface.

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Laroche, Benjamin; Tang, Xinjun; Archer, Gaetan; Di Sanza, Riccardo; Melchiorre, Paolo published the article 《Photochemical chemoselective alkylation of tryptophan-containing peptides》. Keywords: tryptophan peptide photochem chemoselective alkylation light radical precursor; peptide coupling alkylation mechanism enantioselective diastereoselective synthesis.They researched the compound: H-Trp-OMe.HCl( cas:7524-52-9 ).Application of 7524-52-9. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:7524-52-9) here.

We report a photochem. method for the chemoselective radical functionalization of tryptophan (Trp)-containing peptides. The method exploits the photoactivity of an electron donor-acceptor complex generated between the tryptophan unit and pyridinium salts. Irradiation with weak light (390 nm) generates radical intermediates right next to the targeted Trp amino acid, facilitating a proximity-driven radical functionalization. This protocol exhibits high chemoselectivity for Trp residues over other amino acids and tolerates biocompatible conditions.

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1,3-Benzodioxole – Wikipedia,
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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about Fluorescence detected circular dichroism (FDCD) for supramolecular host-guest complexes, the main research direction is cucurbituril paracyclophane inclusion complex mol recognition fluorescence.Category: dioxole.

Fluorescence-detected CD (FDCD) spectroscopy is applied for the first time to supramol. host-guest and host-protein systems and compared to the more known electronic CD (ECD). We find that FDCD can be an excellent choice for common supramol. applications, e.g. for the detection and chirality sensing of chiral organic analytes, as well as for reaction monitoring. Our comprehensive investigations demonstrate that FDCD can be conducted in favorable circumstances at much lower concentrations than ECD measurements, even in chromophoric and auto-emissive biofluids such as blood serum, overcoming the sensitivity limitation of absorbance-based chiroptical spectroscopy. Besides, the combined use of FDCD and ECD can provide addnl. valuable information about the system, e.g. the chem. identity of an analyte or hidden aggregation phenomena. We believe that simultaneous FDCD- and ECD-based chiroptical characterization of emissive supramol. systems will be of general benefit for characterizing fluorescent, chiral supramol. systems due to the higher information content obtained by their combined use.

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1,3-Benzodioxole – Wikipedia,
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Computed Properties of C12H15ClN2O2. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about KI-assisted Sulfur Activation/Insertion/Denitration Strategy towards Dual C-S Bond Formation for One-pot Synthesis of β-Carboline-tethered 2-Acylbenzothiophenes. Author is Singh, Manpreet; Jamra., Rahul; Paul, Avijit K.; Malakar, Chandi C.; Singh, Virender.

A simple and efficient KI promoted sulfur activation-insertion/de-nitration strategy has been developed for the synthesis of β-carboline C1 tethered 2-acylbenzothiophenes via one-pot assembly of 1-acetyl β-carbolines (an alkaloid based scaffold), 2-nitrobenzaldehydes and elemental sulfur. This expeditious reaction proceeds through the formation of β-carboline linked nitro-chalcones followed by embodiment of elemental sulfur to generate the multifunctional β-carboline linked benzothiophene derivatives The highlighted features of this efficient methodol. are transition metal-free conditions, use of inexpensive and non-toxic catalyst, easy procedure, short reaction time, and broad substrate scope with good yields. The scope of this protocol has been extended for the synthesis of a range of novel compounds with significant diversity.

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1,3-Benzodioxole – Wikipedia,
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In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Cu(II)-Catalysed Azide-Alkyne Cycloaddition Reaction towards Synthesis of β-Carboline C1-Tethered 1,2,3-Triazole Derivatives, published in 2021-04-28, which mentions a compound: 7524-52-9, mainly applied to carboline triazole preparation regioselective; alkyne carboline azide cycloaddition reaction copper catalyst, Recommanded Product: H-Trp-OMe.HCl.

The synthesis of hybrid mols. containingβ-carboline C1-linked 1,2,3-triazoles I (R1 = H, COOMe, COOEt; R2 = H, Me, Bn, CH2COOEt, etc.; R3 = Ph, n-Bu, COOEt, n-pentyl, CH2OH; R4 = H, COOEt) in moderate to good yields has been described. The developed transformation was realized by using Cu(II)-catalyzed click-reaction of diverse alkynes R3CC R4 with in-situ derived rarely explored β-carboline tethered aliphatic azides II. These mol. hybrids also exhibited excellent fluorescence properties.

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: H-Trp-OMe.HCl( cas:7524-52-9 ) is researched.Quality Control of H-Trp-OMe.HCl.Martinez-Mingo, Mario; Rodriguez, Nuria; Gomez Arrayas, Ramon; Carretero, Juan C. published the article 《Access to Benzazepinones by Pd-Catalyzed Remote C-H Carbonylation of γ-Arylpropylamine Derivatives》 about this compound( cas:7524-52-9 ) in Organic Letters. Keywords: benzazepinone preparation palladium catalyst gamma arylpropylamine carbonylation. Let’s learn more about this compound (cas:7524-52-9).

A general method for the construction of seven-membered rings through Pd-catalyzed C(sp2)-H carbonylation at the remote ε-position of γ-arylpropylamine derivatives, including chiral α-amino acids, was developed using Mo(CO)6 as the CO source, furnishing richly functionalized benzo[c]azepin-1-one derivatives The readily removable N-SO2Py protecting/directing group provides high levels of chemo-, regio- and diastereoselectivity. Furthermore, this method is amenable to the postsynthetic modification of complex mols. such as small peptides.

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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Enhancement of the chiroptical response of α-amino acids via N-substitution for molecular structure determination using vibrational circular dichroism》. Authors are Polavarapu, Prasad L.; Santoro, Ernesto; Covington, Cody L.; Raghavan, Vijay.The article about the compound:H-Trp-OMe.HClcas:7524-52-9,SMILESS:N[C@@H](CC1=CNC2=CC=CC=C12)C(OC)=O.[H]Cl).Formula: C12H15ClN2O2. Through the article, more information about this compound (cas:7524-52-9) is conveyed.

The chiroptical response in the form of vibrational CD (VCD) in the midinfrared region is found to be enhanced when a hydrogen of amino group of L-tryptophan is substituted with acetyl, acryloyl, or maleyl group. The order of preference for VCD enhancement is found to be acryloyl > acetyl > maleyl group. The resulting exptl. VCD spectra are also found to be satisfactorily reproduced by the quantum mech. (QM) predicted spectra. The QM predicted spectra were simulated using the conformer populations, (a) predicted by Gibbs energies and (b) optimized to maximize the similarity between exptl. and predicted VCD spectra. It is found that the conformer populations predicted by Gibbs energies do not yield the maximum possible similarity between exptl. and the QM predicted spectra. This work identifies the N-substitution of α-amino acids and determining the conformer populations that best reproduce the exptl. spectra as two new approaches for mol. structure determination

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Recommanded Product: 7524-52-9. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about Controlling Size-Dispersion of Single Walled Carbon Nanotubes by Interaction with Polyoxometalates Armed with a Tryptophan Tweezer. Author is Syrgiannis, Zois; Trautwein, Guido; Calvaresi, Matteo; Modugno, Gloria; Zerbetto, Francesco; Carraro, Mauro; Prato, Maurizio; Bonchio, Marcella.

A bis-tryptophan tweezer was installed on a polyoxometalate (POM) surface via a bis-amide covalent bond, yielding the enantiopure hybrid POM with C2 symmetry, as a result of the regioselective functionalization of decatungosilicate [γ-SiW10O36]8- at the lacunary site. The combined polyanionic and receptor properties are instrumental for a POM-driven solubilization and enrichment of single walled C nanotubes (SWCNTs) with diameter < 1.1 nm, as demonstrated by Raman and UV/visible-NIR evidence, in agreement with the calculated energetics of the tryptophan tweezer-SWCNT interaction. Compounds in my other articles are similar to this one(H-Trp-OMe.HCl)Recommanded Product: 7524-52-9, you can compare them to see their pros and cons in some ways,such as convenient, effective and so on.

Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

Polavarapu, Prasad L.; Santoro, Ernesto; Covington, Cody L.; Raghavan, Vijay published the article 《Enhancement of the chiroptical response of α-amino acids via N-substitution for molecular structure determination using vibrational circular dichroism》. Keywords: amino acid mol structure conformer vibrational CD; VCD; amino acids; conformer populations; quantum theoretical calculations; tryptophan.They researched the compound: H-Trp-OMe.HCl( cas:7524-52-9 ).Related Products of 7524-52-9. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:7524-52-9) here.

The chiroptical response in the form of vibrational CD (VCD) in the midinfrared region is found to be enhanced when a hydrogen of amino group of L-tryptophan is substituted with acetyl, acryloyl, or maleyl group. The order of preference for VCD enhancement is found to be acryloyl > acetyl > maleyl group. The resulting exptl. VCD spectra are also found to be satisfactorily reproduced by the quantum mech. (QM) predicted spectra. The QM predicted spectra were simulated using the conformer populations, (a) predicted by Gibbs energies and (b) optimized to maximize the similarity between exptl. and predicted VCD spectra. It is found that the conformer populations predicted by Gibbs energies do not yield the maximum possible similarity between exptl. and the QM predicted spectra. This work identifies the N-substitution of α-amino acids and determining the conformer populations that best reproduce the exptl. spectra as two new approaches for mol. structure determination

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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem