Tag: M.W=150-200

Liu, Jitian published the artcileSynthesis of Lactams via Ir-Catalyzed C-H Amidation Involving Ir-Nitrene Intermediates, COA of Formula: C9H10O3, the main research area is iridium catalyst amidation rearrangement spirocyclization dioxazolone; lactam preparation.

X-membered lactams were synthesized via either an amidation of sp3 C-H bonds or an electrophilic substitution of arenes via Ir-nitrene intermediates. With the employment of a readily available iridium catalyst in dichloromethane or hexafluoro-2-propanol, a wide range of lactams were synthesized in good to excellent yields with high selectivity.

Journal of Organic Chemistry published new progress about Amidation. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, COA of Formula: C9H10O3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Liu, Lulu published the artcileDesign, synthesis and biological evaluation of tyrosine derivatives as Mcl-1 inhibitors, Formula: C9H10O3, the main research area is peptidomimetic tyrosine synthesis drug design apoptosis; mol docking Mcl1 inhibitor peptidomimetic; tyrosine methyl ester bromoalkane condensation benzenesulfonamide amidation coupling; Apoptosis; Cancer; Mcl-1 inhibitors; Tyrosine derivatives.

The upregulation of the protein myeloid cell leukemia-1 (Mcl-1) is closely associated with various human cancers, which can result in the evasion of apoptosis and a low survival rate. Therefore, developing Mcl-1 inhibitors has become a promising paradigm for cancer therapy. Herein, we designed and synthesized a novel series of tyrosine derivatives, among which compounds (I) (R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = OBut, n = 2; R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = Ph, n = 1; R1 = naphthyl, X = Br, R2 = 4-Me-benzyl, n = 1) exhibited very high binding affinity to Mcl-1 with Ki values of 0.18, 0.27 and 0.23μM, resp. Interestingly, compound I (R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = Ph, n = 1) showed not only potent activity against Mcl-1 but also considerable selectivity over Bcl-2 and Bcl-xL, which was rationalized by mol. docking and fragment-centric topog. mapping (FCTM). It is worth noting that compounds I (R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = OBut, n = 2; R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = Ph, n = 1; R1 = naphthyl, X = Br, R2 = 4-Me-benzyl, n = 1) displayed potent antiproliferative activity against several cancer cell lines and could induce apoptosis of KM3 and HepG2 cells in a dose-dependent manner.

European Journal of Medicinal Chemistry published new progress about Amidation. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Formula: C9H10O3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Chen, Wenjun published the artcileSynthesis of benzo[4,5]imidazo[1,2-a]quinoxalines by I2-mediated sp3 C-H amination, Category: isoquinoline, the main research area is benzoimidazoquinoxaline preparation; benzoimidazolyl aniline iodine amination.

Benzo[4,5]imidazo[1,2-a]quinoxaline derivatives were synthesized from readily accessible 2-(benzoimidazol-1-yl)aniline substrates by an I2-mediated direct sp3 C-H amination reaction. This synthetic strategy did not use transition-metals, is operationally simple scalable and gives high yields.

Organic Chemistry Frontiers published new progress about Amination. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Category: isoquinoline.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Ge, Liang published the artcileIron-Catalyzed Radical Acyl-Azidation of Alkenes with Aldehydes: Synthesis of Unsymmetrical β-Azido Ketones, Formula: C11H12O3, the main research area is alkene aldehyde azidotrimethylsilane iron radical acylation azidation catalyst; ketone azido preparation.

An iron-catalyzed acyl-azidation of alkenes under mild reaction conditions has been developed. Aromatic aldehydes or aliphatic aldehydes can be used as the acyl radical precursors; TMSN3 is used as the azido source; TBHP is the initiator. The synthesized unsym. β-azido ketones can be easily transformed into valuable functionalized compounds, such as γ-aminol, γ-azido alc., β-azido oxime, β-azido ester, and triazoles.

Organic Letters published new progress about Acylation. 1205-17-0 belongs to class isoquinoline, name is 2-Methyl-3-(3,4-methylenedioxyphenyl)propionaldehyde, and the molecular formula is C11H12O3, Formula: C11H12O3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Merkens, Kay published the artcileSynthesis of unnatural α-amino acid derivatives via light-mediated radical decarboxylative processes, Product Details of C9H10O3, the main research area is unnatural amino acid synthesis light mediated radical reaction mechanism; chiral dehydroalanine benzylation acylation alkylation carboxylic keto acid decarboxylation.

Unnatural amino acids (UAAs) are key building blocks with widespread application across several scientific fields. Therefore, it is highly attractive to develop straightforward and simple methodologies capable of granting quick access to these species. Herein we report a light-mediated protocol for the synthesis of UAA via radical decarboxylative processes. This methodol., which employs readily available and abundant starting materials – such as carboxylic and α-keto acids – proceeds under very mild reaction conditions and shows a high functional group tolerance. In addition, the products of the radical reaction can be readily derivatized to grant rapid access to complex UAAs.

Advanced Synthesis & Catalysis published new progress about Acylation. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Product Details of C9H10O3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Wang, Shuangshuang published the artcileAmino acid-oriented poly-substituted heterocyclic tetramic acid derivatives as potential antifungal agents, Recommanded Product: 4-Methoxyphenylacetic acid, the main research area is heterocyclic tetramic acid synthesis antifungal agent phytopathogenic fungus; fungicidal structure activity natural product antibiotic thiolactomycin; amino acid phenylacetic esterification acylation amidation Dieckmann cyclocondensation; Antifungal activities; Fungicides; Plant pathogenic fungus; Synthesis; Tetramic acid.

In order to find new potential pesticide mols. with antifungal activities, we have designed and synthesized a series of amino acid-oriented poly-substituted tetramic acid derivatives, and evaluated their potential antifungal activities against six kinds of plant pathogenic fungi commonly found in agriculture systematically, including Phomopsis adianticola, Fusarium graminearum, Alternaria tenuis Nees, Magnaporthe oryzae, Gloeosporium theae-sinensis, Sclerotinia sclerotiorum. According to the preliminary bioassay studies, all tested mols., especially compounds (I) [R1 = H, R2 = H, R3 = Bn, R4 = CO-C(Me,Me)Et; R1 = 2-Me, R2 = H, R3 = Bn, R4 = CO-C(Me,Me)Et; R1 = 2,4-Cl, R2 = H, R3 = CH2SMe, R4 = CO-i-Pr; R1 = H, R2 = 4-i-Pr-C6H5, R3 = Me, R4 = CO-i-Pr] exhibited significant and broad-spectrum anti-fungal effect in vitro compared to the intermediates M-1, M-2, M-3 and hymexazol. What’s more, the inhibition rate of compounds I (R1 = 2-Me, R2 = H, R3 = Bn, R4 = CO-C(Me,Me)Et; R1 = 4-F, R2 = H, R3 = Bn, R4 = CO-i-Pr; R1 = H, R2 = 4-i-Pr-C6H5, R3 = Me, R4 = CO-i-Pr) against Phomopsis adianticola reached 74.42%, 60.33%, 65.21%, as well as compounds I (R1 = R2 = H, R3 = Bn, R4 = CO-OEt; R1 = H, R2 = 4-i-Pr-C6H5, R3 = Me, R4 = CO-i-Pr) against Sclerotinia sclerotiorum were 65.65%, 74.92%, 61.36%. Further investigation results indicated that compounds I [R1 = H, R2 = H, R3 = Bn, R4 = CO-C(Me,Me)Et; R1 = 2-Me, R2 = H, R3 = Bn, R4 = CO-C(Me,Me)Et; R1 = H, R2 = 4-i-Pr-C6H5, R3 = Me, R4 = CO-i-Pr] presented obviously inhibitory activities against Phomopsis adianticola compared with hymexazol, which might be considered as the basic active framework for further potential fungicides discovery.

European Journal of Medicinal Chemistry published new progress about Acylation. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Recommanded Product: 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Arendowski, Adrian published the artcileScreening of urinary renal cancer metabolic biomarkers with gold nanoparticles-assisted laser desorption/ionization mass spectrometry, Computed Properties of 104-01-8, the main research area is gold nanoparticle metabolic biomarker laser desorption ionization mass spectrometry.

Renal cell carcinoma is a very aggressive and often fatal disease for which there are no specific biomarkers found to date. The purpose of this work was to find features that differentiate urine metabolic profiles of healthy people and cancer patients. Laser desorption/ionization mass spectrometry on gold nanostructures-based techniques were used for the metabolic anal. of urine of 50 patients with kidney cancer. Comparison with data from 50 healthy volunteers led to the discovery of several compounds that may be considered potential renal cell carcinoma (RCC) biomarkers. Statistical anal. of data allowed for the discovery of m/z values that had the greatest impact on group differentiation. A database search enabled the assignment of signals for the most promising 15 features among them: serine, heptanol, 3-methyleneindolenine, 2-methyl-3-hydroxy-5-formylpyridine-4-carboxylate, phosphodimethylethanolamine, 4-methoxyphenylacetic acid, N-acetylglutamine, 3,5-dihydroxyphenylvaleric acid, hydroxyhexanoylglycine, valyl-leucine, leucyl-histidine, oleamide, 9,12,13-trihydroxyoctadecenoic acid, stearidonyl carnitine and squalene. Differences of metabolite profiles of human urine could be identified by gold nanoparticle-enhanced target (AuNPET) LDI MS method and used for the detection of renal cancer.

Analytical Sciences published new progress about Biomarkers. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Computed Properties of 104-01-8.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Minic, Jasmina published the artcileFunctional expression of olfactory receptors in yeast and development of a bioassay for odorant screening, HPLC of Formula: 1205-17-0, the main research area is olfactory receptor yeast biosensor odorant screening.

The functional expression of olfactory receptors (ORs) is a primary requirement to examine the mol. mechanisms of odorant perception and coding. Functional expression of the rat I7 OR and its trafficking to the plasma membrane was achieved under optimized exptl. conditions in the budding yeast Saccharomyces cerevisiae. The membrane expression of the receptor was shown by Western blotting and immunolocalization methods. Moreover, we took advantage of the functional similarities between signal transduction cascades of G protein-coupled receptor in mammalian cells and the pheromone response pathway in yeast to develop a novel biosensor for odorant screening using luciferase as a functional reporter. Yeasts were engineered to coexpress I7 OR and mammalian Gα subunit, to compensate for the lack of endogenous Gpa1 subunit, so that stimulation of the receptor by its ligands activates a MAP kinase signaling pathway and induces luciferase synthesis. The sensitivity of the bioassay was significantly enhanced using mammalian Golf compared to the Gα15 subunit, resulting in dose-dependent responses of the system. The biosensor was probed with an array of odorants to demonstrate that the yeast-borne I7 OR retains its specificity and selectivity towards ligands. The results are confirmed by functional expression and bioluminescence response of human OR17-40 to its specific ligand, helional. Based on these findings, the bioassay using the luciferase reporter should be amenable to simple, rapid and inexpensive odorant screening of hundreds of ORs to provide insight into olfactory coding mechanisms.

FEBS Journal published new progress about Biosensors. 1205-17-0 belongs to class isoquinoline, name is 2-Methyl-3-(3,4-methylenedioxyphenyl)propionaldehyde, and the molecular formula is C11H12O3, HPLC of Formula: 1205-17-0.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Alfinito, Eleonora published the artcileSmell Nanobiosensors: Hybrid systems based on the electrical response to odorant capture.Theory And Experiment, Application In Synthesis of 1205-17-0, the main research area is olfactory receptor 17 GPCR rhodopsin nanobiosensor odorant elec impedance.

Mammalian olfactory system is the bio-archetype of smell sensor devices. It is based on a very articulated mechanism which translate the odorant capture information performed by the olfactory receptors (ORs) into a code. Finally, the code is sent to the brain for aroma recognition. Our aim is to partially mimic this system to produce a biosensor on nanometric scale. The active part of the device is constituted of nanosomes containing specific ORs. Each nanosome is interfaced with nanoelectrodes and the odorant capture is converted into an elec. signal. Specifically, the elec. response is correlated with the conformational change that a single OR undergoes when it captures a specific odorant mol. An array of nanodevices should be able to produce specific response profiles. In this paper we present a possible theor. framework in which the exptl. results should be embedded. It consists of the description of the protein in terms of an impedance network able to simulate the elec. characteristics associated with the protein topol. (c) 2009 American Institute of Physics.

AIP Conference Proceedings published new progress about Biosensors. 1205-17-0 belongs to class isoquinoline, name is 2-Methyl-3-(3,4-methylenedioxyphenyl)propionaldehyde, and the molecular formula is C11H12O3, Application In Synthesis of 1205-17-0.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Alfinito, Eleonora published the artcileHuman olfactory receptor 17-40 as an active part of a nanobiosensor: a microscopic investigation of its electrical properties, Safety of 2-Methyl-3-(3,4-methylenedioxyphenyl)propionaldehyde, the main research area is human olfactory receptor nanobiosensor elec resistance impedance spectrum.

Increasing attention has recently been devoted to protein-based nanobiosensors. The main reason is the huge number of possible technol. applications, ranging from drug detection to early cancer diagnosis. Their operating model is based on protein activation and the corresponding conformational change due to the capture of an external mol., the so-called ligand. Recent measurements, performed with different techniques on the human 17-40 olfactory receptor, revealed a very narrow window of response in respect to the odor concentration This is a crucial point for understanding whether the use of this olfactory receptor as a sensitive part of a nanobiosensor is a good choice. In this paper we investigate the topol. and elec. properties of the human olfactory receptor 17-40 with the objective of providing a microscopic interpretation of available experiments To this purpose, we model the protein by means of a graph that is able to capture the mean features of the 3D backbone structure. The graph is then associated with an equivalent impedance network, able to evaluate the impedance spectra of the olfactory receptor in its native and activated state. We assume a topol. origin of the different protein elec. responses to different ligand concentrations: In this perspective all the exptl. data are collected and interpreted satisfactorily within a unified scheme, also useful for application to other proteins.

RSC Advances published new progress about Biosensors. 1205-17-0 belongs to class isoquinoline, name is 2-Methyl-3-(3,4-methylenedioxyphenyl)propionaldehyde, and the molecular formula is C11H12O3, Safety of 2-Methyl-3-(3,4-methylenedioxyphenyl)propionaldehyde.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem