Author: tianli

Zhang, Xiaoxu published the artcileTargeted Delivery of Dasatinib to Deplete Tumor-Associated Macrophages by Mannosylated Mixed Micelles for Tumor Immunotherapy, Formula: C13H15NO6S, the publication is ACS Biomaterials Science & Engineering (2020), 6(10), 5675-5684, database is CAplus and MEDLINE.

Tumor-associated macrophages (TAMs) are abundant in tumors and predominately show protumor M2-type fostering tumor progression. Specific depletion of TAMs is conceivably favorable for antitumor therapy. In this study, mannosylated mixed micelles (DAS-MMic) were developed to specifically deliver dasatinib (DAS) to eliminate TAMs for tumor immunotherapy. In vitro and in vivo results showed that DAS-MMic could effectively eradicate TAMs, decrease angiogenesis, reprogram the immunosuppressive tumor microenvironment, and finally suppress tumor progression. These data suggest the potential of direct elimination of TAMs by DAS-MMic for tumor immunotherapy.

ACS Biomaterials Science & Engineering published new progress about 96345-79-8. 96345-79-8 belongs to alcohols-buliding-blocks, auxiliary class Sugar Units,Gal and Man, name is (2R,3S,4S,5S,6R)-2-(Hydroxymethyl)-6-(4-isothiocyanatophenoxy)tetrahydro-2H-pyran-3,4,5-triol, and the molecular formula is C20H40O2, Formula: C13H15NO6S.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Anderson, Ryan T. published the artcileDirect Conversion of Hydride- to Siloxane-Terminated Silicon Quantum Dots, Related Products of alcohols-buliding-blocks, the publication is Journal of Physical Chemistry C (2016), 120(45), 25822-25831, database is CAplus.

Peripheral surface functionalization of hydride-terminated silicon quantum dots (SiQD) is necessary in order to minimize their oxidation/aggregation and allow for solution processability. Historically thermal hydrosilylation addition of alkenes and alkynes across the Si-H surface to form Si-C bonds has been the primary method to achieve this. The authors demonstrate a mild alternative approach to functionalize hydride-terminated SiQDs using bulky silanols in the presence of free-radical initiators to form stable siloxane (∼Si-O-SiR₃) surfaces with hydrogen gas as a byproduct. This offers an alternative to existing methods of forming siloxane surfaces that require corrosive Si-Cl based chem. with HCl byproducts. A 52 nm blue shift in the photoluminescent spectra of siloxane vs. alkyl-functionalized SiQDs is observed that we explain using computational theory. Model compound synthesis of silane and silsesquioxane analogs is used to optimize surface chem. and elucidate reaction mechanisms. Thorough characterization on the extent of siloxane surface coverage is provided using FTIR and XPS. TEM is used to demonstrate SiQD size and integrity after surface chem. and product isolation.

Journal of Physical Chemistry C published new progress about 597-52-4. 597-52-4 belongs to alcohols-buliding-blocks, auxiliary class Aliphatic Chain, name is Triethylsilanol, and the molecular formula is C6H16OSi, Related Products of alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Cardenas-Castro, Alicia P. published the artcileIn vitro gastrointestinal digestion and colonic fermentation of tomato (Solanum lycopersicum L.) and husk tomato (Physalis ixocarpa Brot.): Phenolic compounds released and bioconverted by gut microbiota, Formula: C8H8O3, the publication is Food Chemistry (2021), 130051, database is CAplus and MEDLINE.

Two of the most important Mexican plant-foods are tomato (Solanum lycopersicum L.) and husk tomato (Physalis ixocarpa Brot.). In this study three objectives were followed: i) to evaluate the bioaccessible phenolic compounds (PC) in T and HT during upper gastrointestinal digestion, ii) to in vitro ferment the indigestible fractions of the samples to evaluate the short-chain fatty acids (SCFA) production, iii) the microbial metabolites, bioconverted PC and volatile organic compounds (VOCs) generated during the fermentation Vanillic acid was the most bioaccessible PC and after 48 h, 3-hydroxyphenylacetic acid was the most abundant microbial metabolite identified in both samples. The identification of VOCs belonging to terpenes (and derivatives) group in T and HT can be product of the microbial metabolism of carotenoids. The study shows new knowledge of the in vitro intestinal digestion and fermentation of T and HT final compounds with biol. potential which should be evaluated in further studies.

Food Chemistry published new progress about 621-37-4. 621-37-4 belongs to alcohols-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Phenol,Natural product, name is 3-Hydroxyphenylacetic acid, and the molecular formula is C8H8O3, Formula: C8H8O3.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Gujar, Jitendra B. published the artcileSynthesis of Dihydropyrano[2,3-C]pyrazoles Using Mandelic Acid as an Efficient Catalyst, Formula: C8H8O3, the publication is Organic Preparations and Procedures International (2022), 54(2), 138-144, database is CAplus.

A simple new synthetic protocol for the preparation of dihydropyrano[2,3-C]pyrazole derivatives I (R = 4-methylphenyl, piperonyl, Et, etc.) using conventional and US methods with green characteristics. The model reaction was performed using one-pot MCR of Et acetoacetate, hydrazine hydrate, p-methylbenzaldehyde RCHO, and malononitrile in water at reflux or US method, using mandelic acid as an efficient catalyst. The considerable advantages of these methods include short reaction times, very good yields, and the avoidance of the use of environmentally hazardous solvents.

Organic Preparations and Procedures International published new progress about 90-64-2. 90-64-2 belongs to alcohols-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Alcohol,Natural product, name is 2-Hydroxy-2-phenylacetic acid, and the molecular formula is C8H8O3, Formula: C8H8O3.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Gudun, Kristina A. published the artcileCobalt-Catalyzed Deoxygenative Hydroboration of Nitro Compounds and Applications to One-Pot Synthesis of Aldimines and Amides, Category: alcohols-buliding-blocks, the publication is Advanced Synthesis & Catalysis (2022), 364(3), 601-611, database is CAplus.

The com. available and bench-stable Co(acac)₂ ligated with bis[(2-diphenylphosphino)phenyl] ether (dpephos) was employed for selective room temperature hydroboration of nitro compounds with HBPin (TOF up to 4615 h^-1), tolerating halide, hydroxy, amino, ether, ester, lactone, amide and heteroaromatic functionalities. These reactions offered a direct access to a variety of N-borylamines RN(H)BPin, which were in situ treated with aldehydes and carboxylic acids to produce a series of aldimines and secondary carboxamides without the need for dehydrating and/or coupling reagents. Combination of these transformations in a sequential one-pot manner allowed for direct and selective synthesis of aldimines and secondary carboxamides from readily available and inexpensive nitro compounds

Advanced Synthesis & Catalysis published new progress about 25240-59-9. 25240-59-9 belongs to alcohols-buliding-blocks, auxiliary class Boronic acid and ester,Boronic Acids,Boronate Esters, name is 4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-ol, and the molecular formula is C6H13BO3, Category: alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Voller, Jiri published the artcile6-Substituted purines as ROCK inhibitors with anti-metastatic activity, Application In Synthesis of 96-20-8, the publication is Bioorganic Chemistry (2019), 103005, database is CAplus and MEDLINE.

Rho-associated serine/threonine kinases (ROCKs) are principal regulators of the actin cytoskeleton that regulate the contractility, shape, motility, and invasion of cells. We explored the relationships between structure and anti-ROCK2 activity in a group of purine derivatives substituted at the C6 atom by piperidin-1-yl or azepan-1-yl groups. Structure-activity relationship (SAR) analyses suggested that anti-ROCK activity is retained, and may be further increased, by substitution of the parent compounds at the C2 atom or by expansion of the C6 side chain. These inhibitors of ROCK can reach effective concentrations within cells, as demonstrated by a decrease in phosphorylation of the ROCK target MLC, and by inhibition of the ROCK-dependent invasion of melanoma cells in the collagen matrix. Our study may be useful for further optimization of C6-substituted purine inhibitors of ROCKs and of other sensitive kinases identified by the screening of a broad panel of protein kinases.

Bioorganic Chemistry published new progress about 96-20-8. 96-20-8 belongs to alcohols-buliding-blocks, auxiliary class Amine,Aliphatic hydrocarbon chain,Alcohol, name is 2-Aminobutan-1-ol, and the molecular formula is C15H14Cl2S2, Application In Synthesis of 96-20-8.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Myers, Richard A. published the artcileα-Conotoxins, small peptide probes of nicotinic acetylcholine receptors, Application In Synthesis of 70539-42-3, the publication is Biochemistry (1991), 30(38), 9370-7, database is CAplus and MEDLINE.

α-Conotoxins, a family of small peptides from the venoms of the Conus marine molluscs, are selective, snake α-neurotoxin-competitive antagonists of the nicotinic acetylcholine receptor. A new α-conotoxin, SIA, has been purified, sequenced, and synthesized. Crosslinking with bivalent reagents and photoaffinity labeling of the acetylcholine receptor with α-conotoxin yield covalent adducts. Surprisingly, crosslinking to other subunits is considerably more efficient than to the α subunit. The relative efficiency of photoactivatable crosslinking to different subunits of the receptor is a function of placement of the photoactivatable group on the toxin. Since the structures of α-conotoxins can be solved by 2D NMR (Pardi, A. et al., 1989 and Kobayashi, Y. et al., 1989) this family of toxins should provide a set of new ligands for probing the acetylcholine receptor with considerable precision.

Biochemistry published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C18H20N2O12, Application In Synthesis of 70539-42-3.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Sinnett-Smith, James published the artcileCharacterization of a bombesin receptor on Swiss mouse 3T3 cells by affinity cross-linking, Quality Control of 70539-42-3, the publication is Journal of Cellular Biochemistry (1988), 38(4), 237-49, database is CAplus and MEDLINE.

A cell surface protein in Swiss 3T3 cells of apparent M_r 75,000-85,000 was identified previously by chem. crosslinking as a major component of the receptor for peptides of the bombesin family in these cells. Because bombesin-like peptides may interact with other cell surface mols., it was important to establish the correlation between receptor binding and functions of this complex and further characterize the M_r 75,000-85,000 cross-linked protein. Detailed time courses carried out at different temperatures demonstrated that the M_r 75,000-85,000 affinity-labeled band was the earliest cross-linked complex detected in Swiss 3T3 cells incubated with ¹²⁵I-labeled gastrin-releasing peptide (¹²⁵I-GRP). Furthermore, the ability of various nonradioactive bombesin agonists and antagonists to block the formation of the M_r 75,000-85,000 cross-linked complex correlated extremely well (r = 0.994) with the relative capacity of these peptides to inhibit ¹²⁵I-GRP specific binding. Pretreatment with unlabeled GRP for up to 6 h caused only a slight decrease in both specific ¹²⁵I-GRP binding and the affinity labeling of the M_r 75,000-85,000 protein. The cross-linked complex is a glycoprotein. First, solubilized affinity labeled M_r 75,000-85,000 complex applied to wheat germ lectin-Sepharose columns was eluted by addition of 0.3M N-acetyl-D-glucosamine. Second, treatment with endo-β-N-acetylglucosaminidase F reduced the apparent mol. weight of the affinity-labeled band from 75,000-85,000 to 43,000, indicating the presence of N-linked oligosaccharide groups.

Journal of Cellular Biochemistry published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C8H14O2, Quality Control of 70539-42-3.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Jeon, Minseok published the artcileStereoselective Synthesis of Cyclohexane Derivatives: Tandem Lithium Iodide Mediated Intramolecular Conjugate Addition of Thiols to α,β-Bisenones, Synthetic Route of 4410-99-5, the publication is Synthesis (2022), 54(12), 2865-2875, database is CAplus.

A tandem intramol. conjugate addition reaction was conducted with α,β-bisenones as selected Michael acceptors which were converted into 1,2,3-trisubstituted six-membered rings in the presence of activated sulfur nucleophiles. The products were obtained in good to excellent yields (maximum yield: 99%). Various substituted α,β-bisenones and sulfur nucleophiles were examined to understand the substrate scope of the reaction. Only one diastereomer was isolated, as lithium iodide mediated enolate trapping reactions improve the stereoselectivity of reactions involving 1,2,3-trisubstituted cyclohexanes.

Synthesis published new progress about 4410-99-5. 4410-99-5 belongs to alcohols-buliding-blocks, auxiliary class Thiol,Benzene, name is 2-Phenylethanethiol, and the molecular formula is C8H10S, Synthetic Route of 4410-99-5.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Zak, Mark published the artcileMinimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors, COA of Formula: C5H10O, the publication is Journal of Medicinal Chemistry (2016), 59(18), 8345-8368, database is CAplus and MEDLINE.

NAMPT inhibitors may show potential as therapeutics for oncol. Throughout our NAMPT inhibitor program, we found that exposed pyridines or related heterocyclic systems in the left-hand portion of the inhibitors are necessary pharmacophores for potent cellular NAMPT inhibition. However, when combined with a benzyl group in the center of the inhibitors, such pyridine-like moieties also led to consistent and potent inhibition of CYP2C9. In an attempt to reduce CYP2C9 inhibition, a parallel synthesis approach was used to identify central benzyl group replacements with increased Fsp3. A spirocyclic central motif was thus discovered that was combined with left-hand pyridines (or pyridine-like systems) to provide cellularly potent NAMPT inhibitors with minimal CYP2C9 inhibition. Further optimization of potency and ADME properties led to the discovery of compound 68, a highly potent NAMPT inhibitor with outstanding efficacy in a mouse tumor xenograft model and lacking measurable CYP2C9 inhibition at the concentrations tested.

Journal of Medicinal Chemistry published new progress about 20117-47-9. 20117-47-9 belongs to alcohols-buliding-blocks, auxiliary class Aliphatic cyclic hydrocarbon,Alcohol, name is 1-Methylcyclobutan-1-ol, and the molecular formula is C4H12ClNO, COA of Formula: C5H10O.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts