201037-95-8

Upstream product

• 18162-48-6 tert-butyldimethylsilyl chloride 
• 112-27-6 2,2'-[1,2-ethanediylbis(oxy)]bisethanol 

Downstream Products

• 109-16-0 triethyleneglycol dimethacrylate 
• 495417-68-0 2-[2-[2-[(tert-butyldimethylsilyl)oxy]ethoxy]ethoxy]ethyl methacrylate 
• 943601-23-8 N-(2-[2-{2-hydroxyethoxy}ethoxy]ethyl)-2-nitro-benzenesulfonamide 
• 943601-24-9 (2-[2-azidoethoxy]ethyl)-N-nosylethanamine 
• 943601-78-3 tert-butyl (2-(2-(2-(2-nitrophenylsulfonamido)ethoxy)ethoxy)ethyl)carbamate 
• 943601-30-7 C₃₇H₄₉F₃N₁₀O₁₁S₂ 
• 943601-31-8 C₃₁H₄₆F₃N₉O₇S 
• 199484-66-7 toluene-4-sulfonic acid 2-{2-[2-(tert-butyl-dimethyl-silanyloxy)-ethoxy]-ethoxy}-ethyl ester 
• 6338-55-2 2-(2-(2-aminoethoxy)ethoxy)ethan-1-ol 
• 1447810-65-2 (E)-8,8-bis(phenylsulfonyl)-12-hydroxy-1,14,17-trioxacyclononadecan-10-en-2-one 
• 1447810-59-4 7,7-bis(phenylsulfonyl)heptanoic acid 2-[2-(3-vinyloxiranylmethoxy)ethoxy]ethyl ester 
• 208827-90-1 O-propargyl triethylene glycol 
• 943601-22-7 C₁₈H₃₂O₇SiSN₂ 

Relevant academic research and scientific papers

Total synthesis of a biotinylated derivative of phorboxazole A via Sonogashira coupling

The C46 terminus of phorboxazole A has been modified to incorporate a biotin-terminated linker via direct palladium-mediated Sonogashira reaction conditions. Synthetic 45,46-dehydrobromophorboxazole A was joined with a tris-(polyethyleneglycol)vinyl iodid

Prodrug compound and application ofprodrug compound in treatment of cancer

The present invention provides a compound indicated by a formula (I), pharmaceutically acceptable salts or esters thereof, a pharmaceutical composition of the compound, and application of the compoundand the pharmaceutical composition in the inhibition or regulation of the activity of tyrosine kinase and treating disease symptoms or symptoms including cancer mediated by tyrosine kinase.

PRODRUGS OF THE TYROSINE KINASE INHIBITOR FOR TREATING CANCER

There are provided compounds of Formula (I), and pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions thereof, useful for inhibition or modulation of the activity of tyrosine kinases and treatment of disease states or conditions mediated by tyrosine kinases, including cancers. (I)

ALKYNYL INDAZOLE DERIVATIVE AND USE THEREOF

The main object of the present invention is to provide a novel compound which has a VEGF receptor tyrosine kinase inhibitory activity and is useful as an active ingredient for the treatment of diseases accompanying angiogenesis or edema, for example, age-related macular degeneration or the like. The present invention includes, for example, an alkynyl indazole derivative represented by the following general formula (I), a pharmaceutical acceptable salt thereof, and a medicine containing thereof.

INHIBITORS OF HEPATITIS C VIRUS POLYMERASE

The present invention provides, among other things, compounds represented by the general Formula I: (I) and pharmaceutically acceptable salts thereof, wherein L and A (and further substituents) are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.

BCR-ABL TYROSINE-KINASE LIGANDS CAPABLE OF DIMERIZING IN AN AQUEOUS SOLUTION, AND METHODS OF USING SAME

Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. invivo) to form a multimer (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding sites on a Bcr-Abl tyrosine kinase.

Hexanes/acetonitrile: A binary solvent system for the efficient monosilylation of symmetric primary and secondary diols

Symmetric diols are useful compounds in the synthesis of natural products, their value often dependent on their successful monoprotection. A general and simple method for the monosilylation of symmetrical primary and secondary diols is reported. The metho

Investigation of the origin and synthetic application of the pseudodilution effect for Pd-catalyzed macrocyclisations in concentrated solutions with immobilized catalysts

Immobilized Pd-complexes allowed macrocyclisations via the Tsuji-Trost-reaction in concentrated solutions. Systematic studies suggest that the origin of this pseudodilution effect is neither film diffusion nor gel diffusion, but the reduction in conformational freedom of intermediates and intramolecular prenucleophile activation. In contrast a pseudodilution effect could not be observed for Sonogashira- and Suzuki-macrocyclisations.

Synthesis and evaluation of cardiac glycoside mimics as potential anticancer drugs

The cardiac glycoside digitoxin, consisting of a steroid core linked to a labile trisaccharide, has been used for centuries for the treatment of congestive heart failure. The well known pharmacological effect is a result of the ability of cardiac glycosides to inhibit the Na+, K +-ATPase. Within recent years cardiac glycosides have furthermore been suggested to possess valuable anticancer activity. To mimic the labile trisaccharide of digitoxin with a stabile carbohydrate surrogate, we have used sulfur linked ethylene glycol moieties of varying length (mono-, di-, tri- or tetra-ethylene glycol), and furthermore used these linkers as handles for the synthesis of bivalent steroids. The prepared compounds were evaluated for their potencies to inhibit the Na+, K+-ATPase and for their cytotoxic effect on cancerous MCF-7 cells. A clear trend is observed in both inhibition and cytotoxic effect, where the bioactivity decreases as the size increases. The most potent Na+, K+-ATPase inhibitors are the compounds with the shortest ethylene glycol chain (Kapp 0.48 μM) and thiodigitoxigenin (Kapp 0.42 μM), which both are comparable with digitoxigenin (Kapp 0.52 μM). For the cancer cell viability assay the shortest mimics were found to have highest efficacy, with the best ligand having a monoethylene glycol unit (IC50 0.24 μM), which was slightly better than digitoxigenin (IC50 0.64 μM), while none of the novel cardiac glycoside mimics display an in vitro effect as high as digitoxin (IC50 0.02 μM).

Water-soluble nile blue derivatives: syntheses and photophysical properties

Four water-soluble 2-hydroxy-Nile Blue derivatives, 1a, 1b, 2a, and 2b, were prepared by condensation reactions performed under relatively mild conditions (90°C, N,N-dimethylformamide with no added acid). These fluorescent probes had more favorable fluorescence characteristics than two known water-soluble Nile Blue derivatives. Specifically, they were superior to the known dyes with respect to their quantum yields in aqueous media and the sharpness of their fluorescence emissions. Concentration-dependant UV absorption and fluorescence emission studies indicated that the dyes did not aggregate in aqueous solution at concentrations of less than 1-4 μM. The new water-soluble materials 1a, 1b, 2a, and 2b emit in a desirable region of the fluorescence spectrum (A = 670-675 nm). Overall they are potentially interesting for labeling biomolecules in aqueous environments.