Month: December 2022

Kim, Eun-Young published the artcileBLT2 promotes the invasion and metastasis of aggressive bladder cancer cells through a reactive oxygen species-linked pathway, Formula: C12H23N3S, the publication is Free Radical Biology & Medicine (2010), 49(6), 1072-1081, database is CAplus and MEDLINE.

Aggressive bladder cancer is a major cause of morbidity and mortality. Despite the fact that metastatic disease results in death in the majority of bladder cancer cases, the mol. events regulating the invasive phenotype of aggressive bladder cancer are not well understood. In this study, immunohistochem. examination showed that the leukotriene B₄ receptor BLT2 is overexpressed in advanced malignant bladder cancers (human transitional cell carcinomas) in proportion to advancing stages, with high prognostic significance (p < 0.001). Blockade of BLT2 with the specific antagonist LY255283 or siRNA knockdown significantly suppressed the invasiveness of highly aggressive 253 J-BV bladder cancer cells. Moreover, our results demonstrated that BLT2 mediates invasiveness through a signaling pathway dependent on NAD(P)H oxidase (Nox) 1- and Nox4-induced generation of reactive oxygen species (ROS) and subsequent NF-κB stimulation. Metastasis of 253 J-BV cells in mice was also dramatically suppressed by inhibition of BLT2 or its signaling. These findings suggest that a BLT2-Nox-ROS-NF-κB cascade plays a critical role in bladder cancer invasion and metastasis.

Free Radical Biology & Medicine published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Formula: C12H23N3S.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Kim, Jun published the artcileLong-Term Anti-Inflammatory effects of injectable celecoxib nanoparticle hydrogels for achilles tendon regeneration., Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Acta Biomaterialia (2022), 183-194, database is CAplus and MEDLINE.

The treatment of chronic Achilles tendonitis (AT) often requires prolonged therapy and invasive therapeutic methods such as surgery or therapeutic endoscopy. To prevent the progression of chronic AT, excessive inflammation must be alleviated at an early stage. Corticosteroids or nonsteroidal anti-inflammatory drugs are generally prescribed to control inflammation; however, the high doses and long therapeutic periods required may lead to serious side effects. Herein, a local injectable poly(organophosphazene) (PPZ) – celecoxib (CXB) nanoparticle (PCNP) hydrogel system with long-term anti-inflammatory effects was developed for the treatment of tendonitis. The amphiphilic structure and thermosensitive mech. properties of PPZ means that the hydrophobic CXB can be easily incorporated into the hydrophobic core to form PCNP at 4°C. Following the injection of PCNP into the AT, PCNP hydrogel formed at body temperature and induced long-term local anti-inflammatory effects via sustained release of the PCNP. The therapeutic effects of the injectable PCNP system can alleviate excessive inflammation during the early stages of tissue damage and boost tissue regeneration. This study suggests that PCNP has significant potential as a long-term anti-inflammatory agent through sustained nonsteroidal anti-inflammatory drugs (NSAIDs) delivery and tissue regeneration boosting. In the treatment of Achilles tendinitis, a long-term anti-inflammatory effect is needed to alleviate excessive inflammation and induce regeneration of the damaged Achilles tendon. Injectable poly(organophosphazene)(PPZ)-celecoxib(CXB) nanoparticles (PCNP) generated a long-term, localized-anti-inflammatory effect in the injected region, which successfully induced the expression of anti-inflammatory cytokines and suppressed pro-inflammatory cytokines, while the PCNPs degraded completely. Accordingly, regeneration of the damaged Achilles tendon was achieved through the long-term anti-inflammatory effect induced by a single PCNP injection. The PCNP system therefore has great potential in long-term NSAIDs delivery for various tissue engineering applications.

Acta Biomaterialia published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, Recommanded Product: 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Paul, Alexis published the artcileCombining G-quadruplex targeting motifs on a single peptide nucleic acid scaffold: a hybrid (3 + 1) PNA-DNA bimolecular quadruplex, Application In Synthesis of 186046-83-3, the publication is Chemistry – A European Journal (2008), 14(28), 8682-8689, database is CAplus and MEDLINE.

We describe the 1st G-quadruplex targeting approach that combines intercalation and hybridization strategies by investigating the interaction of a G-rich peptide nucleic acid (PNA) acridone conjugate with a 3-repeat fragment of the human telomere G3 to form a hybrid PNA-DNA quadruplex that mimics the biol. relevant (3 + 1) pure DNA dimeric telomeric quadruplex. Using a combination of UV and fluorescence spectroscopy, CD, and mass spectrometry, we show that PNA can induce the formation of a bimol. hybrid quadruplex even at low salt concentration upon interaction with a single-stranded 3-repeat fragment of telomeric DNA. However, PNA cannot invade a short fragment of B-DNA even if the latter contains a CCC motif complementary to the PNA sequence. These studies could open up new possibilities for the design of a novel generation of quadruplex ligands that target not only the external features of the quadruplex but also its central core constituted by the tetrads themselves.

Chemistry – A European Journal published new progress about 186046-83-3. 186046-83-3 belongs to amides-buliding-blocks, auxiliary class Purine,Carboxylic acid,Amine,Benzene,Amide,Others,PNA,, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, and the molecular formula is C40H35N7O8, Application In Synthesis of 186046-83-3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Anilkumar, Gopinadhan N. published the artcileII. Novel HCV NS5B polymerase inhibitors: discovery of indole C2 acyl sulfonamides, COA of Formula: C7H8FNO2S, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(1), 713-717, database is CAplus and MEDLINE.

Development of SAR at the C2 position of indole lead I, a palm site inhibitor of HCV NS5B polymerase (NS5B IC₅₀ = 0.053 μM, replicon EC₅₀ = 4.8 μM), is described. Initial screening identified an acyl sulfonamide moiety as an isostere for the C2 carboxylic acid group. Further SAR investigation resulted in identification of acyl sufonamide analog II (NS5B IC₅₀ = 0.039 μM, replicon EC₅₀ = 0.011 μM) with >100-fold improved replicon activity.

Bioorganic & Medicinal Chemistry Letters published new progress about 489-17-8. 489-17-8 belongs to amides-buliding-blocks, auxiliary class Fluoride,Sulfamide,Amine,Benzene, name is 4-Fluoro-2-methylbenzenesulfonamide, and the molecular formula is C7H8FNO2S, COA of Formula: C7H8FNO2S.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Thorat, Kishor G. published the artcilePyrrole-thiazole based push-pull chromophores: An experimental and theoretical approach to structural, spectroscopic and NLO properties of the novel styryl dyes, Quality Control of 14294-10-1, the publication is Journal of Photochemistry and Photobiology, A: Chemistry (2017), 1-17, database is CAplus.

Novel push-pull fluorophores constituted by two donors (substituted pyrrole and morpholine) linked to acceptor through thiazole electron spacer have been synthesized. The fluorophores are investigated for linear and non-linear optical properties by UV-VIS absorption and fluorescence spectroscopies, and by means of TD-DFT (B3LYP/6-31G(d)) method, with the aim of elucidating the ability of the morpholine/pyrrole-donor-thiazole-spacer based D-π-A fluorophores as organic NLO materials. The bond length alternation and generalized Mulliken-Hush (GMH) anal. is performed to understand the involvement of the donor in effective transfer of the charge to acceptor. Values of first-order hyperpolarizabilities (β_CT or β₀), obtained by the solvatochromic method (Lippert Mataga model), and the transition dipole moments (μ_eg) used to characterize and evaluate the non-linear optical performances of the D-π-A fluorophores in various microenvironments. The D-π-A fluorophores possess good values of β_CT or β₀ in different organic solvents and hold high thermal stabilities therefore can be used as potential organic NLO materials.

Journal of Photochemistry and Photobiology, A: Chemistry published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C12H17NS2, Quality Control of 14294-10-1.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Tayade, Rajratna P. published the artcileSynthesis of Novel Thiazole Based Carbaldehyde as Potential Sensor for Fluoride Anion and their Spectroscopic Properties, Safety of Morpholine-4-carbothioamide, the publication is Journal of Fluorescence (2017), 27(3), 1117-1128, database is CAplus and MEDLINE.

A novel thiazole based carbaldehyde bearing benzimidazole fluorophore as the receptor unit for F^– anion was prepared by multistep synthesis. D. functional theory was used to understand the structural and electronic properties of the receptor. The anion sensing activities of receptor I were studied for various anions in acetonitrile solvent. The receptor showed fluorescence enhancement in the presence of fluoride anion due to intramol. charge transfer (ICT) mechanism. No significant changes were observed upon addition of less basic anions such as OAc^–, Cl^–, Br^–, I^–, HSO₄^–. After the interaction of fluoride anion with the receptor I leads to an 88 nm red shift in emission maxima. [TBA]OH and ¹H NMR titration experiments indicated that deprotonation of N-H in the benzimidazole due to interaction with fluoride anions.

Journal of Fluorescence published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C10H10O2, Safety of Morpholine-4-carbothioamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Tayade, Rajratna P. published the artcileNovel Thiazole Based Styryl Dyes with Benzimidazole Unit – Synthesis, Photophysical and TD-DFT Studies, COA of Formula: C5H10N2OS, the publication is Journal of Fluorescence (2017), 27(1), 167-180, database is CAplus and MEDLINE.

Three new Y-shaped styryl dyes were designed and synthesized from thiazole carbaldehyde with different active methylene compounds as acceptor moieties. All the dyes were characterized by IR, ¹HNMR, MS/LCMS/HRMS. Spectroscopic properties and non-linear optical properties styryl derivatives were analyzed and the effect of change in solvent polarity on their absorption and emissive properties has been investigated. The dye with (1-phenylethylidene) propanedinitrile unit shows red shift absorption/emission profile among all the dyes. D. Functional Theory and Time Dependent-D. Functional Theory computations have been used for comparative study with the exptl. data and also to understand the structural, mol., electronic and photophys. parameters of the styryl dyes. The computational method was also employed to investigate the nonlinear optical properties of the styryl dyes in different organic solvent. The unsubstituted benzimidazolyl thiazole styryl dyes possess good non-linear optical properties.

Journal of Fluorescence published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C6H12O2, COA of Formula: C5H10N2OS.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Shreykar, Milind R. published the artcileResonance induced proton transfer leading to NIR emission in coumarin thiazole hybrid dyes: Synthesis and DFT insights, Application of Morpholine-4-carbothioamide, the publication is Tetrahedron Letters (2016), 57(37), 4174-4177, database is CAplus.

Two novel coumarin thiazole hybrid dyes (E)-2-(3-(2-(4-(4-hydroxy-2-oxo-2H-chromen-3-yl)-2-morpholinothiazol-5-yl)vinyl)-5,5-dimethylcyclohex-2-en-1-ylidene)malononitrile (CSI) and (E)-2-(3-(2-(4-(4-methoxy-2-oxo-2H-chromen-3-yl)-2-morpholinothiazol-5-yl)vinyl)-5,5-dimethylcyclohex-2-en-1-ylidene)malononitrile (MeOCSI) were synthesized. CSI exhibits near IR emission with large Stokes shift. The dye CSI shows resonance induced excited state intramol. proton transfer (RI-ESIPT). DFT and TD-DFT calculations clearly support and define the finding.

Tetrahedron Letters published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C3H3Br2ClO, Application of Morpholine-4-carbothioamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Holm, Regina published the artcileMultifunctional Cationic PeptoStars as siRNA Carrier: Influence of Architecture and Histidine Modification on Knockdown Potential, Product Details of C11H22N2O4, the publication is Macromolecular Bioscience (2020), 20(1), 1900152, database is CAplus and MEDLINE.

RNA interference provides enormous potential for the treatment of several diseases, including cancer. Nevertheless, successful therapies based on siRNA require overcoming various challenges, such as poor pharmacokinetic characteristics of the small RNA mol. and inefficient cytosolic accumulation. In this respect, the development of functional siRNA carrier systems is a major task in biomedical research. To provide such a desired system, the synthesis of 3-arm and 6-arm PeptoStars is aimed for. The different branched polypept(o)idic architectures share a stealth-like polysarcosine corona for efficient shielding and a multifunctional polylysine core, which can be independently varied in size and functionality for siRNA complexation-, transport and intra cellular release. The special feature of star-like polypept(o)ides is in their uniform small size (<20 nm) and a core-shell structure, which implies a high stability and stealth-like properties and thus, they may combine long circulation times and a deep penetration of cancerous tissue. Initial toxicity and complement studies demonstrate well tolerated cationic PeptoStars with high complexation capability toward siRNA (N/P ratio up to 3:1), which can lead to potent RNAi for optimized systems. Here, the synthetic development of 3-arm and 6-arm polypept(o)idic star polymers, their modification with endosomolytic moieties, and first in vitro insights on RNA interference are reported on.

Macromolecular Bioscience published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Product Details of C11H22N2O4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Zigeuner, G. published the artcileHeterocycles, part 51. Syntheses of 4-dialkylamino-5,6-dihydro-2(1H)-pyridinethiones and 4-alkylamino or 4-arylamino compounds, Related Products of amides-buliding-blocks, the publication is Monatshefte fuer Chemie (1976), 107(6), 1361-7, database is CAplus.

(Dialkylamino)dihydro-2(1H)-pyridinethiones I (R = Me or R2 = CH2CH2OCH2CH2) were prepared by heating the heterocycles II (X = NH, S) with dialkylformamides or by the reaction of secondary amines with thiazinthiones III (R1 = OH, morpholino), with MeCOCH2CMe2NHCSNR2 or with MeCOCH2CMe2N:C:S. A general method for the preparation of I is the reaction of R2NH.HNCS, R2NCSNH2, or dialkylammonium chlorides and KCNS with MeCOCH:CHMe or MeCOCH2CH2OH.

Monatshefte fuer Chemie published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C7H16Cl2Si, Related Products of amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics