83405-98-5

Upstream product

• 159191-56-7 (4-((tert-butyldimethylsilyl)oxy)phenyl)boronic acid 
• 94-18-8 Benzyl 4-hydroxybenzoate 
• 18162-48-6 tert-butyldimethylsilyl chloride 
• 138585-08-7 (4-((tert-butyldimethylsilyl)oxy)phenyl)methanol 
• 124-38-9 carbon dioxide 
• 1188303-92-5 tert-butyl (4-(5,5-dimethyl-1,3,2-dioxaborinan-2-yl)phenoxy)dimethylsilane 
• 99-96-7 4-hydroxy-benzoic acid 
• 78324-14-8 tert-butyldimethylsilyl 4-((tert-butyldimethylsilyl)oxy)benzoate 
• 288-32-4 1H-imidazole 

Downstream Products

• 1355681-25-2 (8R)-(3'R-hydroxy-5'R-(4-hydroxybenzoyloxy)-6'S-methyl-(2H)-tetrahydropyran-2'-yloxy)non-(2E)-enoic acid 
• 1449688-60-1 C₂₅H₂₈BrNO₆Si 
• 90446-67-6 4-((tert-butyldimethylsilyl)oxy)benzoyl chloride 
• 1449688-61-2 C₂₀H₁₃⁽³⁾H₃BrNO₆ 
• 1450590-56-3 C₁₈H₉⁽³⁾H₃BrNO₆ 
• 155204-26-5 4-fluoro-N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-pyridin-2-ylbenzylamide 

Relevant academic research and scientific papers

One-step modification to identify dual-inhibitors targeting both pancreatic triglyceride lipase and Niemann-Pick C1-like 1

Pancreatic triglyceride lipase (PTL) and Niemann-Pick C1-like 1 (NPC1L1) have been identified as attractive therapeutic targets for obesity and hypercholesteremia, respectively. Obesity and hypercholesteremia usually co-exist, however no dual-inhibitors against PTL and NPC1L1 were reported for the treatment of obesity patients with hypercholesteremia so far. In this work, molecular hybridization-based one-step modification screening identified a potent dual-inhibitor against PTL and NPC1L1. Compound P1-11 has IC50 values of 2.1 μM against PTL through covalent binding, as well as significantly reduces cholesterol absorption in a non-competitive inhibitory manner. Molecule docking and molecular dynamics studies revealed the reason of its activity to both PTL and NPC1L1. Moreover, the gene and protein expression levels of PTL and NPC1L1 were also determined respectively after the treatment of P1-11. Development of dual-inhibitors against PTL and NPC1L1 could provide novel treatment options for obesity patients with hypercholesteremia. The results of current research would great support the development of dual-inhibitors against PTL and NPC1L1.

Cell sugar transport channel inhibitor

The invention discloses a cell sugar transport channel inhibitor of which the structure is shown as a formula (I). The cell sugar transport channel inhibitor disclosed by the invention can target a cell sugar transport channel, and inhibit tumor cell prol

Tumor diagnosis and treatment fluorescent probe for targeting tumor Wolburg effect

The invention discloses a tumor diagnosis and treatment fluorescent probe for targeting tumor Warburg effect, and the structure of the fluorescent probe is shown as a formula (I). The fluorescent probe can be directly used in a cell line to analyze and detect the expression degree of tumor cell GLUT1 protein, so as to complete the screening of tumor cells. Meanwhile, tumor cell proliferation is inhibited by directly blocking the GLUT1 channel to inhibit intake of sugar nutritional ingredients by tumors. And an effective means and a useful tool are provided for early screening and diagnosis oftumors, development of new anti-tumor drugs and the like.

COMPOSITIONS AND METHODS FOR MAKING HYBRID POLYPEPTIDES

Compositions and methods of making hybrid polypeptides and other polymers are disclosed. For example, functionalized tRNA having a functional molecule including a benzoic acid or benzoic acid derivative acylated to the 3' nucleotide of a tRNA are provided

Composition, thermal conductive sheet, the thermally conductive layer with a device (by machine translation)

The film thickness of the thermal conductivity sheet having thermal conductivity [to] direction forming a composition. Also, in the film thickness direction of the heat conductive sheet having excellent thermal conductivity, the thermal conductivity sheet

Capping Strategies for Covalent Template-Directed Synthesis of Linear Oligomers Using CuAAC

Covalent templating provides an attractive solution to the controlled synthesis of linear oligomers because a template oligomer can be used to define the precise length and sequence of the product. If the monomer units are attached to the template using kinetically inert covalent bonds it should be possible to operate at high dilution to favor intramolecular over intermolecular reaction. However, for oligomerization reactions using copper-catalyzed azide alkyne cycloaddition (CuAAC) this is not the case. The rate-limiting step is formation of an activated copper complex, so any alkyne that is activated by copper reacts rapidly with the nearest available azide. As a result, every time a chain end alkyne is activated, rapid intermolecular reaction takes place with a different oligomer leading to the formation of higher order products. It proved possible to block these intermolecular reactions by adding an excess of an azide capping agent that intercepts the chain end of the growing oligomer on the template. By adjusting the concentration of the capping agent to compete effectively with the unwanted intermolecular reactions without interfering with the desired intramolecular reactions, it was possible to obtain quantitative yields of copy strands from covalent template-directed oligomerization reactions. Remarkably, the capping agent could also be used to control the stereochemistry of the duplex formed in the templated oligomerization reaction to give exclusively the antiparallel product.

Expedient Synthesis of Alphitolic Acid and Its Naturally Occurring 2- O-Ester Derivatives

The expedient synthesis of alphitolic acid (1) as well as its natural C-3-epimer and 2-O-ester derivatives was accomplished in a few steps from the readily commercially available betulin (9). A Rubottom oxidation delivered an α-hydroxy group in a stereo- and chemoselective manner. The diastereoselective reduction of the α-hydroxy ketone was key to accessing the 1,2-diol moiety of this class of natural products. Our concise and stereoselective synthetic protocol allowed the gram-scale synthesis of these natural products, which will facilitate future biological evaluations.

Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning

Potent covalent inhibitors of Bruton's tyrosine kinase (BTK) based on an aminopyrazole carboxamide scaffold have been identified. Compared to acrylamide-based covalent reactive groups leading to irreversible protein adducts, cyanamide-based reversible-covalent inhibitors provided the highest combined BTK potency and EGFR selectivity. The cyanamide covalent mechanism with BTK was confirmed through enzyme kinetic, NMR, MS, and X-ray crystallographic studies. The lead cyanamide-based inhibitors demonstrated excellent kinome selectivity and rat pharmacokinetic properties.

Galloyl esters of trans-stilbenes are inhibitors of FASN with anticancer activity on non-small cell lung cancer cells

Fatty acid synthase (FASN) is a lipogenic enzyme that is selectively upregulated in malignant cells. There is growing consensus on the oncogenicity of FASN-driven lipogenesis and the potential of FASN as a druggable target in cancer. Here, we report the synthesis and FASN inhibitory activities of two novel galloyl esters of trans-stilbene EC1 and EC5. Inhibition of FASN was accompanied by a loss in AKT activation and profound apoptosis in several non-small cell lung cancer (NSCLC) cells at the growth inhibitory concentrations of EC1 and EC5. Both FASN and phospho-AKT levels were concurrently downregulated. However, addition of a lipid concentrate to the treated cells reinstated cell viability and reversed the loss of FASN and AKT protein levels, thus recapitulating the causal relationship between FASN inhibition and the loss in cell viability.

Bis(methoxypropyl) ether-promoted oxidation of aromatic alcohols into aromatic carboxylic acids and aromatic ketones with O2 under metal- and base-free conditions

We describe an eco-friendly, practical and operationally simple procedure for the bis(methoxypropyl) ether-promoted oxidation of aromatic alcohols into aromatic carboxylic acids and aromatic ketones with atmospheric dioxygen as the sole oxidant. This chemical process is clean with high conversion and good selectivity, and an external initiator, catalyst, additive and base are not required. The virtue of this reaction is highlighted by its easily available and economical raw materials and excellent functional group tolerance (acid-, base- and oxidant-labile groups).