Day: October 14, 2022

Huang, Zhiyong; Wang, Dan; Long, Cheng-Yu; Li, Shen-Huan; Wang, Xue-Qiang; Tan, Weihong published the artcile< Regulating the Anticancer Efficacy of Sgc8-Combretastatin A4 Conjugates: A Case of Recognizing the Significance of Linker Chemistry for the Design of Aptamer-Based Targeted Drug Delivery Strategies>, Recommanded Product: 1,2-Di(pyridin-2-yl)disulfane, the main research area is aptamer targeted drug delivery anticancer efficacy cytotoxicity cell viability.

The unique merits of aptamers, including specificity, high binding affinity, easy cell internalization, and rapid tissue accumulation abilities, have led aptamer-drug conjugates to evolve into one of the most attractive strategies for targeted drug delivery purposes. Nevertheless, the critical role of linkers in regulating anticancer efficacy of these conjugates, especially those engineered by automated modular synthesis techniques, has been rarely explored. In this work, we utilized Sgc8c aptamer and combretastatin A4 to develop three conjugates with either a phosphodiester bond linker, a disulfide bond linker, or a carbamate linker to study their payload release mechanisms and the influence on anticancer efficacy. These investigations allowed us to identify the unique activation pathway of the phosphodiester bond linker that is activated by both nucleophilic attack of glutathione and degradation caused by phosphodiesterase, which is highly associated with the higher cytotoxicity of the conjugate. Importantly, the understanding of the chem. of phosphodiester bond linker activation allowed us to further design another XQ-2d-CA4 conjugate that can induce pancreatic cancer cells apoptosis in a more efficient manner.

Journal of the American Chemical Society published new progress about Antitumor agents. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Recommanded Product: 1,2-Di(pyridin-2-yl)disulfane.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mittelbach, Martin published the artcile< An easy and convenient synthesis of 6-methyl-4(1H)-pyridone-3-carboxylic acid>, Reference of 86129-63-7, the main research area is nicotinic acid dihydro oxo methyl.

The title acid (I) was prepared from a nicotinic acid derivative Et 2,4-dichloro-6-methylnicotinate was treated with Na and R1OH (R1 = Me, Et), the alkoxy analog products II were subjected to reductive dechlorination, and the products were hydrolyzed by HCl to give I.

Synthesis published new progress about 86129-63-7. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, Reference of 86129-63-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Dedeian, K.; Djurovich, P. I.; Garces, F. O.; Carlson, G.; Watts, R. J. published the artcile< A new synthetic route to the preparation of a series of strong photoreducing agents: fac-tris-ortho-metalated complexes of iridium(III) with substituted 2-phenylpyridines>, Related Products of 370878-69-6, the main research area is photoreducing agent phenylpyridine iridium complex; pyridylbenzene iridium complex.

Reaction of 2-phenylpyridine (Hppy) with Ir(acac)3 (acac = acetylacetonato) in refluxing glycerol gives the fac-tris-ortho-metalate of Ir(III), fac-Ir(ppy)3 in high yield (45%). Phenyl-ring-substituted derivatives of 2-phenylpyridine (R-Hppy) were prepared by cross-coupling of 2-bromopyridine with substituted bromobenzenes. These react with Ir(acac)3 in a manner analogous to Hppy to give similarly high yields (40-75%) of their resp. tris-ortho-metalates, fac-Ir(R-ppy)3.

Inorganic Chemistry published new progress about Electrochemistry. 370878-69-6 belongs to class pyridine-derivatives, and the molecular formula is C33H21F3IrN3, Related Products of 370878-69-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kalindjian, S. Barret; Kadnur, Sanjay V.; Hewson, Christopher A.; Venkateshappa, Chandregowda; Juluri, Suresh; Kristam, Rajendra; Kulkarni, Bheemashankar; Mohammed, Zainuddin; Saxena, Rohit; Viswanadhan, Vellarkad N.; Aiyar, Jayashree; McVey, Donna published the artcile< A New Series of Orally Bioavailable Chemokine Receptor 9 (CCR9) Antagonists; Possible Agents for the Treatment of Inflammatory Bowel Disease>, Quality Control of 56622-54-9, the main research area is dioxoisoindoline derivative preparation CCR9 antagonist inflammatory bowel disease pharmacokinetics.

Chemokine receptor 9 (CCR9), a cell surface chemokine receptor which belongs to the G protein-coupled receptor, 7-trans-membrane superfamily, is expressed on lymphocytes in the circulation and is the key chemokine receptor that enables these cells to target the intestine. It has been proposed that CCR9 antagonism represents a means to prevent the aberrant immune response of inflammatory bowel disease in a localized and disease specific manner and one which is accessible to small mol. approaches. One possible reason why clin. studies with vercirnon, a prototype CCR9 antagonist, were not successful may be due to a relatively poor pharmacokinetic (PK) profile for the mol. We wish to describe work aimed at producing new, orally active CCR9 antagonists based on the 1,3-dioxoisoindoline skeleton. This study led to a number of compounds that were potent in the nanomolar range and which, on optimization, resulted in several possible preclin. development candidates with excellent PK properties.

Journal of Medicinal Chemistry published new progress about Anti-inflammatory agents. 56622-54-9 belongs to class pyridine-derivatives, and the molecular formula is C7H10N2, Quality Control of 56622-54-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hao, Shu-Yi; Qi, Zhi-Yuan; Wang, Shuai; Wang, Xing-Rong; Chen, Shi-Wu published the artcile< Synthesis and bioevaluation of N-(3,4,5-trimethoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-amines as tubulin polymerization inhibitors with anti-angiogenic effects>, Related Products of 777931-67-6, the main research area is pyridopyrazole trimethoxyaniline palladium acetate catalyst haloalkane Buchwald Hartwig coupling; trimethoxyphenyl pyrazolo pyridinamine preparation antitumor cytotoxicity SAR; Aniogenesis; Antitumor; Inhibitors; Pyrazolo[3,4-b]pyridine; Tubulin polymerization.

A new series of N-(3,4,5-trimethoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-amine derivatives I [R1 = H, Me, cyclopentyl; R2 = Me, Et, Pr, etc.] as tubulin polymerization inhibitors were synthesized, and evaluated for the anti-proliferative activities. A structure-activity relationship study revealed that the free amino moiety of 1H-pyrazolo[3,4-b]pyridin-3-amine played an essential role in the anti-proliferative activities. Especially, compound I [R1 = H; R2 = methyl] displayed the strongest anti-proliferation against MCF-7 cells with IC50 value of 0.067 ± 0.003μM, and high selectivity over the normal human embryonic lung WI-38 cells with IC50 value of 23.41 ± 1.53μM. Further mechanistic studies revealed that I [R1 = H; R2 = methyl] showed strong anti-tubulin polymerization activity, changed the morphol. of tubulin, and arrested the cell cycle at the G2/M transition in MCF-7 cells. Mol. docking anal. suggested that I [R1 = H; R2 = methyl] well occupied the colchicine-binding pocket of tubulin. Addnl., I [R1 = H; R2 = methyl] demonstrated anti-angiogenic activities with blocking the migration, invasion and tube formation, disrupting the newly formed tube, and regulating both MMP-9 and TIMP-1 in HUVEC cells. In summary,results highlight that compound I [R1 = H; R2 = methyl] was a potential antitumor compound that was worthy of further development.

Bioorganic & Medicinal Chemistry published new progress about Antiangiogenic agents. 777931-67-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrClNO, Related Products of 777931-67-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Herrera, Christian Leonardo; Santiago, Joao Victor; Pastre, Julio Cezar; Correia, Carlos Roque Duarte published the artcile< In Tandem Auto-Sustainable Enantioselective Heck-Matsuda Reactions Directly from Anilines>, Computed Properties of 1416819-91-4, the main research area is aniline cyclopentenol palladium catalyst enantioselective Heck Matsuda reaction green; phenyl cyclopentenol preparation; cyclopentenedicarboxylate aniline palladium catalyst enantioselective Heck Matsuda reaction green; dimethyl phenyl cyclopentenedicarboxylate preparation; butenediol aniline palladium catalyst enantioselective Heck Matsuda reaction green; aryl furanone preparation.

An in tandem enantioselective Heck-Matsuda (HM) reaction of cyclic and acyclic olefins directly from anilines was described. The method relied on a process involving the progressive in situ diazotization of the starting anilines followed by a palladium-catalyzed Heck-Matsuda arylation using chiral N,N-ligands. This intermol. enantioselective HM arylation strategy was applied to the desymmetrization of three distinct unactivated olefins as proof of concept. The method demonstrates broad substrate scope furnishing the Heck adducts in good to excellent enantiomeric ratios of up to 99:1, high diastereoselectivities (cyclopenten-3-ol with>20:1 dr), and good overall yields of up to 82% over 2 or 3 steps.

Advanced Synthesis & Catalysis published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 1416819-91-4 belongs to class pyridine-derivatives, and the molecular formula is C13H15F3N2O, Computed Properties of 1416819-91-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Chhem-Kieth, Sorivan; Lametsch, Rene; Hansen, Erik Torngaard; Ruiz-Carrascal, Jorge published the artcile< Storage and thermal stability of novel heme-based pigments prepared from porcine hemoglobin>, Product Details of C7H7NO2, the main research area is porcine Hb heme pigment storage thermal stability.

The stability of novel meat pigments derived from heme-enriched extract obtained from porcine Hb was assessed. Four different ligands (sodium nitrite, 4-methylimidazole, Me nicotinate, and pyrazine) were used to produce spray-dried, microencapsulated heme-ligand complexes. The storage and thermal stabilities of the produced pigments were assessed, over a 6-mo storage period and across a temperature range of 25-75°C. Color measurements and evaluation were made on the dissolved pigments by UV-visible absorbance spectroscopy and CIELAB color space. All heme-ligand complexes exhibited a stable red color across the storage period, except for the heme-Me nicotinate adduct, which color faded to brown after 30 days of storage. For thermal stability, only the heme-4-methylimidazole complex did not retain its red color beyond 55°C. The redness of the heme-pyrazine complex showed improvement upon heating, which is proposed to be due to the degradation of polymeric heme-pyrazine structure formed during the ligation process. Due to the global effort to reduce nitrite addition in food product, there is an important interest to replace it in processed meat products, wholly or in part. Addnl., the perspective of optimizing the usage of an under-utilized blood fraction is attractive for the meat industry. The development of a heme pigment derived from porcine blood thus presents a good com. potential. Two important aspects of such product would be its stability upon storage, or during heat treatment to levels similar to what is used in processed, cooked meat products. This study presents the behavior for those two aspects of different heme-ligand complexes, and compares the results obtained with a heme pigment produced from the traditionally used nitrite.

Journal of Food Process Engineering published new progress about Blood. 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Product Details of C7H7NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Gonzalez, Alexandre; Benfodda, Zohra; Benimelis, David; Fontaine, Jean-Xavier; Molinie, Roland; Meffre, Patrick published the artcile< Extraction and Identification of Volatile Organic Compounds in Scentless Flowers of 14 Tillandsia Species Using HS-SPME/GC-MS>, Electric Literature of 93-60-7, the main research area is Tillandsia volatile organic compound flower mass spectrometry; PCA analysis; Tillandsia; faint-scented flowers; gas chromatography-mass spectrometry (GC-MS); headspace solid phase microextraction (HS-SPME); heatmap; scentless flowers; volatile organic compounds (VOCs).

VOCs emitted by flowers play an important role in plant ecol. In the past few years, the Tillandsia genus has been scarcely studied according to the VOCs emitted by flowers. Hence, we decided to enlarge the VOCs composition study already undergone in our laboratory on fragrant 3 Tillandsia species to 12 unscented and 2 faint-scented Tillandsia species and hybrids. The headspace solid phase microextraction (HS-SPME) coupled with gas chromatog. combined with the mass spectrometry (GC-MS) method was used to explore the chem. diversity of the VOCs. This study allowed the identification of 65 VOCs among the 14 species and between 6 to 25 compounds were identified in each of the species. The aromatic profile of 10 of the species and hybrids are similar to each other′s and show 8 predominant compounds: benzaldehyde, benzacetaldehyde, hexanol, hexanal, heptanal, octanal, nonanal, and furan-2-pentyl. Some specific compounds are present only in some unique species such as trans-calamenene, α-muurolene, and α-guaiene trans-β-bergamotene. The two faint-scented species studied present an original aromatic profile with a high number of monoterpenes or phenylpropanoids/benzenoids. Our studies allow a better understanding of the ecol. role and function of these VOCs in the interactions between these plants with their environment.

Metabolites published new progress about Aliphatic alcohols Role: ANT (Analyte), BSU (Biological Study, Unclassified), PAC (Pharmacological Activity), THU (Therapeutic Use), ANST (Analytical Study), BIOL (Biological Study), USES (Uses). 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Electric Literature of 93-60-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Liu, Ya-Nan; Hou, Jin-Le; Wang, Zhi; Gupta, Rakesh Kumar; Jaglicic, Zvonko; Jagodic, Marko; Wang, Wen-Guang; Tung, Chen-Ho; Sun, Di published the artcile< An Octanuclear Cobalt Cluster Protected by Macrocyclic Ligand: In Situ Ligand-Transformation-Assisted Assembly and Single-Molecule Magnet Behavior>, Quality Control of 366-18-7, the main research area is octanuclear cobalt silsesquioxane sandwich cluster preparation crystal mol structure; hexamethylcyclohexasiloxanolate cobalt octanuclear sandwich preparation single mol magnet; protected macrocyclic ligand transformation assisted mol magnet behavior.

Macrocyclic mols. with multiple coordination sites have been widely used as promising ligands to build polynuclear metal clusters; however, cyclic silsesquioxane-based metal clusters are still rare. Herein, authors report a new octanuclear Co-silsesquioxane cluster [Co8(OH)2{(MeSiO2)6}2(bpy)2(Obpy)2] (SD/Co8c; SD = SunDi), wherein the Co8 disk-like core is sandwiched by two hexamethylcyclohexasiloxanolate ligands (MeSiO2)6 at two poles and finally encircled by two bpy (bpy = 2,2′-bipyridine) and two Obpy (HObpy = 6-hydroxy-2,2′-bipyridine) ligands at the equatorial region. Interestingly, both MeSi(OMe)3 and bpy undergo in situ transformations to generate hexameric cyclic (MeSiO2)6 and Obpy, resp. The unusual hydroxylation of bpy and the OH- anion in the center of Co8 core provide addnl. binding sites to induce the formation of the larger cluster instead of the traditional hexanuclear cluster. The solution stability and fragmentation route in the gas phase were studied by cold-spray ionization and collision-induced dissociation mass spectrometry, resp. Both results reveal that the Co8 core is quite stable in solution as well as in the gas phase, even with increased collision voltage. Magnetic susceptibility studies of SD/Co8c show the slow magnetization relaxation indicative of single-mol. magnet (SMM) behavior. This work not only presents the multiple in situ ligand-transformation-assisted assembly of polynuclear cobalt cluster but also provides some new insights into the magnetism-structure relationship for SMMs.

Inorganic Chemistry published new progress about Crystal structure. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Quality Control of 366-18-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Izzo, Francesco; Mercurio, Mariano; de Gennaro, Bruno; Aprea, Paolo; Cappelletti, Piergiulio; Dakovic, Aleksandra; Germinario, Chiara; Grifa, Celestino; Smiljanic, Danijela; Langella, Alessio published the artcile< Surface modified natural zeolites (SMNZs) as nanocomposite versatile materials for health and environment>, COA of Formula: C21H38ClN, the main research area is zeolite nanocomposite ibuprofen sodium salt drug release surface modification; Bayesian information criterion; Emerging contaminant; Ibuprofen; NSAID; Nižný hrabovec; Non-linear regression; Sips; Surfactant; Toth; Zeolite.

The present research deals with the evaluation of a clinoptilolite-rich rock, occurring in the Nizny ‘Hrabovec deposit (Slovakia), for high-value technol. applications based on sorption and in vitro release of nonsteroidal anti-inflammatory drugs (i.e., ibuprofen sodium salt). This georesource was surface modified (SMNZ) using four cationic surfactants. Results demonstrate that ibuprofen sorption is very fast and SMZNs can sorb up to ~26 mg/g of drug as a function of the type of counterion and morphol. of surfactant, as well as the hydrophobicity and mol. structure of the drug. Maximum sorption capacities observed for all SMNZs are fully comparable to other adsorbent carriers usually used for removal of contaminants in wastewaters. Sorption of ibuprofen is controlled by a dual mechanism: external anionic exchange and partition into the hydrophobic portion of the patchy bilayer. A prompt drug release in simulated intestinal fluid (SIF) was also observed, making this natural material also suitable to provide rapid soothing effects in potential pharmacol. applications. Comparing the results of this study with other recent investigations, a good technol. performance of clinoptilolite-rich rock can be inferred despite the relatively low zeolite content (~56 weight%).

Colloids and Surfaces, B: Biointerfaces published new progress about Adsorption. 123-03-5 belongs to class pyridine-derivatives, and the molecular formula is C21H38ClN, COA of Formula: C21H38ClN.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem