Day: October 12, 2022

Marson, Charles M.; Matthews, Christopher J.; Yiannaki, Elena; Atkinson, Stephen J.; Soden, Peter E.; Shukla, Lena; Lamadema, Nermina; Thomas, N. Shaun B. published the artcile< Discovery of Potent, Isoform-Selective Inhibitors of Histone Deacetylase Containing Chiral Heterocyclic Capping Groups and a N-(2-Aminophenyl)benzamide Binding Unit>, Product Details of C10H11NS2, the main research area is aminophenylbenzamide pyrimidine imidazolinone thiazoline capped preparation histone deacetylase inhibition; thiazoline capped HDAC3 NCoR1 inhibitor preparation antitumor activity apoptosis.

The synthesis of a novel series of potent chiral inhibitors of histone deacetylase (HDAC) is described that contain a heterocyclic capping group and a N-(2-aminophenyl)benzamide unit that binds in the active site. In vitro assays for the inhibition of HDAC1, HDAC2, HDAC3-NCoR1, and HDAC8 by the N-(2-aminophenyl)benzamide I gave resp. IC50 values of 930, 85, 12, and 4100 nM, exhibiting class I selectivity and potent inhibition of HDAC3-NCoR1. Both imidazolinone and thiazoline rings are shown to be effective replacements for the pyrimidine ring present in many other 2-(aminophenyl)benzamides previously reported, an example of each ring system at 1 μM causing an increase in histone H3K9 acetylation in the human cell lines Jurkat and HeLa and an increase in cell death consistent with induction of apoptosis. Inhibition of the growth of MCF-7, A549, DU145, and HCT116 cell lines by I was observed, with resp. IC50 values of 5.4, 5.8, 6.4, and 2.2 mM.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Product Details of C10H11NS2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Wu, Yikang; Sun, Ya-Ping; Yang, Yong-Qing; Hu, Qi; Zhang, Qi published the artcile< Removal of thiazolidinethione auxiliaries with benzyl alcohol mediated by DMAP>, SDS of cas: 171877-39-7, the main research area is acylthiazolidinethione benzyl alc substitution DMAP; benzyl ester preparation; DMAP substitution mediator.

In the presence of DMAP, a range of N-acylthiazolidinethiones carrying different substituents were smoothly converted into benzyl esters, e.g., I. All the benzyl esters were obtained in good yields.

Journal of Organic Chemistry published new progress about Aldol condensation, stereoselective. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, SDS of cas: 171877-39-7.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Zambito, Giorgia; Gaspar, Natasa; Ridwan, Yanto; Hall, Mary P.; Shi, Ce; Kirkland, Thomas A.; Encell, Lance P.; Loewik, Clemens; Mezzanotte, Laura published the artcile< Evaluating Brightness and Spectral Properties of Click Beetle and Firefly Luciferases Using Luciferin Analogues: Identification of Preferred Pairings of Luciferase and Substrate for In Vivo Bioluminescence Imaging>, Name: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is beetle firefly luciferase dentification bioluminescence imaging; Bioluminescence; Emission spectrum; In vivo imaging; Luciferase; Luciferin.

Currently, a variety of red and green beetle luciferase variants are available for bioluminescence imaging (BLI). In addition, new luciferin analogs providing longer wavelength luminescence have been developed that show promise for improved deep tissue imaging. However, a detailed assessment of these analogs (e.g., Akalumine-HCl, CycLuc1, and amino naphthyl luciferin (NH2-NpLH2)) combined with state of the art luciferases has not been performed. The aim of this study was to evaluate for the first time the in vivo brightness and spectral characteristics of firefly (Luc2), click beetle green (CBG99), click beetle red 2 (CBR2), and Akaluc luciferases when paired with different D-luciferin (D-LH2) analogs in vivo. Transduced human embryonic kidney (HEK 293T) cells expressing individual luciferases were analyzed both in vitro and in mice (via s.c. injection). Following introduction of the luciferins to cells or animals, the resulting bioluminescence signal and photon emission spectrum were acquired using a sensitive charge-coupled device (CCD) camera equipped with a series of band pass filters and spectral unmixing software. Our in vivo anal. resulted in four primary findings: (1) the best substrate for Luc2, CBG99, and CBR2 in terms of signal strength was D-luciferin; (2) the spectra for Luc2 and CBR2 were shifted to a longer wavelength when Akalumine-HCl was the substrate; (3) CBR2 gave the brightest signal with the near-IR substrate, NH2-NpLH2; and (4) Akaluc was brighter when paired with either CycLuc1 or Akalumine-HCl when paired with D-LH2. We believe that the exptl. results described here should provide valuable guidance to end users for choosing the correct luciferin/luciferase pairs for a variety of BLI applications.

Molecular Imaging and Biology published new progress about Bioluminescence. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Name: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Gou, Xue-Ya; Zhang, Bo-Sheng; Wang, Xin-Gang; Shi, Wei-Yu; Liu, Hong-Chao; An, Yang; Zhang, Zhe; Liang, Yong-Min published the artcile< Visible-light-induced ligand-free RuCl3 catalyzed C-H phosphorylation in water>, Name: Ethyl 4-methylthiazole-5-carboxylate, the main research area is light ruthenium photocatalyst phosphorylation water green chem arene heteroarene; crystal structure mol phosphine oxide preparation green chem organophosphorus.

Visible-light-induced C-H phosphorylation of para-CAr-H and heteroarenes was realized using cost-effective RuCl3 as a catalyst. The reaction conditions are green and environmentally friendly, using water as a solvent at room temperature and without ligands. A broad range of highly functional organophosphorus compounds were obtained via a cross-dehydrogenation-coupling (CDC) reaction. In addition, we also proved that RuCl3 is a photocatalyst via its absorption spectrum and on/off light experiments

Chemical Communications (Cambridge, United Kingdom) published new progress about Crystal structure. 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Name: Ethyl 4-methylthiazole-5-carboxylate.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Potewar, Taterao M.; Ingale, Sachin A.; Srinivasan, Kumar V. published the artcile< Catalyst-free efficient synthesis of 2-aminothiazoles in water at ambient temperature>, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is bromomethyl aryl ketone substituted thiourea heterocyclization catalyst free; aryl aminothiazole fanetizole preparation.

A highly efficient and facile method has been described for the synthesis of substituted 2-aminothiazoles, e.g., I, in water without any added catalyst or co-organic solvent. The reaction was carried out at ambient temperature and the products were obtained in excellent isolated yields. The developed protocol is successfully applied for the preparation of an anti-inflammatory drug, fanetizole.

Tetrahedron published new progress about Alkyl aryl ketones Role: RCT (Reactant), RACT (Reactant or Reagent) (bromo). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Hoseinzadeh, A. R.; Javadpour, S. published the artcile< Electrochemical, thermodynamic and theoretical study on anticorrosion performance of a novel organic corrosion inhibitor in 3.5% NaCl solution for carbon steel>, SDS of cas: 96-53-7, the main research area is carbon steel sodium chloride corrosion inhibitor electrochem anticorrosion property.

The theor. and electrochem. performance of a novel organic corrosion inhibitor 3,4-dihydro-3-[2-mercaptothiazolidine]indol-2-one (DMI), for API 5L Grade B carbon steel in 3.5% NaCl, was evaluated by potentiodynamic polarization (Tafel), electrochem. impedance spectroscopy (EIS) and d. functional theory (DFT) for quantum chem. studies. Potentiodynamic studies confirmed that DMI was a mixed organic corrosion inhibitor type which specially affects the cathodic branch. The inhibition efficiencies of reactants, DMI and acetylcysteine followed the following order at 25oC and 200 ppm: DMI (87%) > isatin (71%) > 2-thiazoline-2-thiol (62%) > acetylcysteine (54%). EIS measurements illustrated the charge transfer controlled corrosion process. The Langmuir adsorption isotherm model of DMI was adopted. Surface studies were performed using SEM. Activation and adsorption thermodn. parameters of DMI were computed. The magnitude of ΔGoads and the sign of ΔHoads concluded that the adsorption occurred through chemisorption. Quantum chem. calculations of four corrosion inhibitors were used for investigating the mol. structure effect on inhibition efficiency.

Bulletin of Materials Science published new progress about Adsorption. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, SDS of cas: 96-53-7.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Peixoto, Philippe A.; Richard, Jean-Alexandre; Severin, Rene; Chen, David Y.-K. published the artcile< Total Synthesis of Echinopines A and B: Exploiting a Bioinspired Late-Stage Intramolecular Cyclopropanation>, Related Products of 171877-39-7, the main research area is echinopine A B synthesis intramol cyclopropanation.

Total synthesis of echinopine A and B have been accomplished, based on a strategy that involved two transition-metal-mediated ene-yne cycloisomerizations. A modified Pd-catalyzed enyne cycloisomerization/intramol. Diels-Alder cascade rendered a more streamlined synthesis of tricyclic ketone I, and a Ru-catalyzed ene-yne cycloisomerization/cyclopropanation resembled the late-stage [5/7] → [3/5/5/7] ring-forming sequence in the proposed biosynthetic pathway.

Organic Letters published new progress about Cycloisomerization. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Related Products of 171877-39-7.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Patel, Vimal I.; Patel, Harsha U.; Patel, Chhaganbhai N.; Suthar, Kiran J. published the artcile< Synthesis and anti-bacterial study of 4-(4-substituted phenyl)-5,6-disubstituted-1-(4-substituted phenylthiazol-2-yl)pyridin-2(1H)-one>, Reference of 57493-24-0, the main research area is pyridinone arylthiazolyl preparation antibacterial.

4-(4-Substituted phenyl)-5,6-disubstituted-1-(4-substituted phenylthiazol-2-yl)pyridin-2(1H)-ones have been prepared from citric acid. It is treated with concentrate H2SO4 and then with phenetole to give β-arylglutaconic acid which on fusion with 2-amino 4-substituted phenylthiazole gave 4-(substituted phenyl)-1-1(4-substituted phenylthiazol-2-yl)pyridine-2,6(1H,3H)-dione. Then reaction with phosphorus oxychloride gave 5,6-dichloro-4-(4-substituted phenyl)-1-(4-substituted phenylthiazol-2-yl)pyridin-2(1H)-one. This, on treatment with secondary amines, yields 4-(4-substituted phenyl)-5,6-disubstituted-1-(4-substituted-phenylthiazol-2-yl)pyridin-2(1H)-one. All the title compounds characterized on the basis of their IR, MASS, 1H NMR spectroscopic data anal.

Asian Journal of Research in Chemistry published new progress about Antibacterial agents. 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Reference of 57493-24-0.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Wang, Yixuan; Chen, Quan; Wu, Di; Chen, Qifeng; Gong, Guanghui; He, Liuqing; Wu, Xiaoying published the artcile< Lamin-A interacting protein Hsp90 is required for DNA damage repair and chemoresistance of ovarian cancer cells>, Category: thiazole, the main research area is laminA protein Hsp DNA damage chemoresistance ovarian cancer cell.

Ovarian cancer is the most malignant gynecol. cancer. Previous studies found that lamin-A was associated with DNA damage repair proteins but the underlying mechanism remains unclear. We speculate that this may be related to its interacting proteins, such as Hsp90. The aim of this study is to investigate the effects of Hsp90 on DNA damage repair and chemoresistance of ovarian cancer cells. In our research, co-immunoprecipitation (co-IP) and mass spectrometry (MS) were used to identify proteins interacting with lamin-A and the interaction domain. Next, the relationship between lamin-A and Hsp90 was explored by Western blotting (WB) and immunofluorescence staining. Then, effect of Hsp90 inhibition on DNA damage repair was assessed through detecting Rad50 and Ku80 by WB. Furthermore, to test the roles of 17-AAG on cell chemosensitivity, CCK-8 and colony formation assay were carried out. Meanwhile, IC50 of cells were calculated, followed by immunofluorescence to detect DNA damage. At last, the mouse xenograft model was used in determining the capacity of 17-AAG and DDP to suppress tumor growth and metastatic potential. The results showed that lamin-A could interact with Hsp90 via the domain of lamin-A1-430. Besides, the distribution of Hsp90 could be affected by lamin-A. After lamin-A knockdown, Hsp90 decreased in the cytoplasm and increased in the nucleus, suggesting that the interaction between lamin-A and Hsp90 may be related to the nucleocytoplasmic transport of Hsp90. Moreover, inhibition of Hsp90 led to an obvious decrease in the expression of DSBs (DNA double-strand break) repair proteins, as well as cell proliferation ability upon DDP treatment and IC50 of DDP, causing more serious DNA damage. In addition, the combination of 17-AAG and DDP restrained the growth of ovarian cancer efficiently in vivo and prolonged the survival time of tumor-bearing mice.

Cell Death & Disease published new progress about Antitumor agents. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Category: thiazole.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Pola, Robert; Kral, Vlastimil; Filippov, Sergey K.; Kaberov, Leonid; Etrych, Tomas; Sieglova, Irena; Sedlacek, Juraj; Fabry, Milan; Pechar, Michal published the artcile< Polymer Cancerostatics Targeted by Recombinant Antibody Fragments to GD2-Positive Tumor Cells>, SDS of cas: 96-53-7, the main research area is polymer tumor targeting antibody ganglioside GD2.

A water-soluble polymer cancerostatic actively targeted against cancer cells expressing a disialoganglioside antigen GD2 was designed, synthesized and characterized. A polymer conjugate of an antitumor drug doxorubicin with a N-(2-hydroxypropyl)methacrylamide-based copolymer was specifically targeted against GD2 antigen-pos. tumor cells using a recombinant single chain fragment (scFv) of an anti-GD2 monoclonal antibody. The targeting protein ligand was attached to the polymer-drug conjugate either via a covalent bond between the amino groups of the protein using a traditional nonspecific aminolytic reaction with a reactive polymer precursor or via a noncovalent but highly specific interaction between bungarotoxin covalently linked to the polymer and the recombinant scFv modified with a C-terminal bungarotoxin-binding peptide. The GD2 antigen binding activity and GD2-specific cytotoxicity of the targeted noncovalent polymer-scFv complex proved to be superior to the covalent polymer-scFv conjugate.

Biomacromolecules published new progress about Antibody-drug conjugates. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, SDS of cas: 96-53-7.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica