Tosyl compounds are organic derivatives characterized by the introduction of a tosyl group, which is the sulfonate ester of p-toluenesulfonic acid (CH3C6H4SO3H), into an organic molecule through a substitution reaction.

Androgen-independent induction of prostate-specific antigen gene expression via cross-talk between the androgen receptor and protein kinase A signal transduction pathways. (1/409)

Transcription of the prostate-specific antigen (PSA) gene escapes regulation by androgens in advanced prostate cancer. To determine the molecular mechanism(s) of androgen-independent regulation of the PSA gene, the possibility that the androgen receptor (AR) is activated in the absence of androgen by stimulation of protein kinase A (PKA) was investigated. Activation of PKA by forskolin resulted in elevated expression of the PSA gene in androgen-depleted LNCaP cells, an effect that was blocked by the antiandrogen, bicalutamide. Further evidence that induction of PSA gene expression was dependent on AR was obtained from experiments using PC3 cells devoid of AR. Neither PSA, PB, nor ARR3 androgen-responsive reporters could be induced by activation of PKA in the absence of transfected AR. In addition, when nuclear AR from forskolin-treated LNCaP cells was incubated with oligonucleotides encoding an androgen response element of the PSA promoter and examined by electromobility shift assay, an increase in AR-androgen response element complex formation was observed. Lastly, cotransfection of an expression vector for a chimeric protein encoding the amino-terminal domain of the human AR linked to Gal4 and a 5xGal4UAS reporter gene construct resulted in activation of the amino-terminal domain of the AR by stimulation of PKA activity. These results demonstrate androgen-independent induction of PSA gene expression in prostate cancer cells by an AR-dependent pathway.  (+info)

Lack of effect of zafirlukast on the pharmacokinetics of azithromycin, clarithromycin, and 14-hydroxyclarithromycin in healthy volunteers. (2/409)

This randomized, open-label, crossover study was conducted to investigate whether the coadministration of zafirlukast would affect the pharmacokinetics of azithromycin, clarithromycin, or 14-hydroxyclarithromycin (14-OHC). Twelve healthy subjects (six males and six females) received single 500-mg doses of azithromycin and clarithromycin with and without zafirlukast given to a steady-state concentration. Blood was collected prior to all macrolide doses and for 3 and 10 days after each clarithromycin and azithromycin dose, respectively. Serum was assayed for azithromycin, clarithromycin, and 14-OHC concentrations by validated high-performance liquid chromatography assay systems. Data analyses were done by noncompartmental and nonparametric methods. Analysis of the patients indicated that the addition of steady-state concentrations of zafirlukast did not significantly alter the pharmacokinetic parameters of or overall exposure (based on the area under the concentration-time curve) to azithromycin, clarithromycin, and 14-OHC. While zafirlukast is a known inhibitor of CYP3A4, it does not appear to exert a clinically or statistically significant pharmacokinetic effect on azithromycin, clarithromycin, or 14-OHC.  (+info)

Histochemically reactive zinc in plaques of the Swedish mutant beta-amyloid precursor protein transgenic mice. (3/409)

Endogenous metals such as zinc may contribute to beta-amyloid (Abeta) aggregation and hence the plaque formation. In the present study, we examined brains of four Swedish mutant amyloid precursor protein (APP) transgenic mice at 12 months of age for histochemically reactive zinc in the plaques. Here, we report that all the Congo red (+) mature plaques contained chelatable zinc, as demonstrated by staining with the zinc-specific fluorescent dye 6-methoxy-8-quinolyl-para-toluenesulfonamide (TSQ). On the other hand, Congo red (-) preamyloid Abeta deposits were not stained with TSQ. Interestingly, although cerebellum contained similar degree of preamyloid Abeta deposits as cerebral cortex, it was completely devoid of Congo red- or TSQ-stained mature plaques. Although zinc from plaques was only slowly and partially removed by a specific zinc remover, dithizone, treatment of brain sections with heparinase-III, which degrades heparan sulfate proteoglycan (HSPG), another major constituent of plaques, greatly fastened the zinc removal with dithizone. The present study has demonstrated the presence of histochemically reactive zinc in plaques, but not preamyloid Abeta deposits, of the Swedish mutant APP transgenic mice. Because preamyloid Abeta deposits fail to develop into congophilic plaques in cerebellum where synaptic vesicle zinc is deficient, the synaptic zinc may be a necessary element in the plaque formation. In holding zinc inside plaques, HSPG may contribute in addition to Abeta.  (+info)

Selection for androgen receptor mutations in prostate cancers treated with androgen antagonist. (4/409)

The role of androgen receptor (AR) mutations in androgen-independent prostate cancer (PCa) was determined by examining AR transcripts and genes from a large series of bone marrow metastases. Mutations were found in 5 of 16 patients who received combined androgen blockade with the AR antagonist flutamide, and these mutant ARs were strongly stimulated by flutamide. In contrast, the single mutant AR found among 17 patients treated with androgen ablation monotherapy was not flutamide stimulated. Patients with flutamide-stimulated AR mutations responded to subsequent treatment with bicalutamide, an AR antagonist that blocks the mutant ARs. These findings demonstrate that AR mutations occur in response to strong selective pressure from flutamide treatment.  (+info)

Switch from antagonist to agonist of the androgen receptor bicalutamide is associated with prostate tumour progression in a new model system. (5/409)

Advanced prostate cancer is treated by androgen ablation and/or androgen receptor (AR) antagonists. In order to investigate the mechanisms relevant to the development of therapy-resistant tumours, we established a new tumour model which closely resembles the situation in patients who receive androgen ablation therapy. Androgen-sensitive LNCaP cells were kept in androgen-depleted medium for 87 passages. The new LNCaP cell subline established in this manner, LNCaP-abl, displayed a hypersensitive biphasic proliferative response to androgen until passage 75. Maximal proliferation of LNCaP-abl cells was achieved at 0.001 nM of the synthetic androgen methyltrienolone (R1881), whereas 0.01 nM of this compound induced the same effect in parental cells. At later passages (> 75), androgen exerted an inhibitory effect on growth of LNCaP-abl cells. The non-steroidal anti-androgen bicalutamide stimulated proliferation of LNCaP-abl cells. AR protein expression in LNCaP-abl cells increased approximately fourfold. The basal AR transcriptional activity was 30-fold higher in LNCaP-abl than in LNCaP cells. R1881 stimulated reporter gene activity in LNCaP-abl cells even at 0.01 nM, whereas 0.1 nM of R1881 was needed for induction of the same level of reporter gene activity in LNCaP cells. Bicalutamide that acts as a pure antagonist in parental LNCaP cells showed agonistic effects on AR transactivation activity in LNCaP-abl cells and was not able to block the effects of androgen in these cells. The non-steroidal AR blocker hydroxyflutamide exerted stimulatory effects on AR activity in both LNCaP and LNCaP-abl cells; however, the induction of reporter gene activity by hydroxyflutamide was 2.4- to 4-fold higher in the LNCaP-abl subline. The changes in AR activity were associated neither with a new alteration in AR cDNA sequence nor with amplification of the AR gene. Growth of LNCaP-abl xenografts in nude mice was stimulated by bicalutamide and repressed by testosterone. In conclusion, our results show for the first time that the nonsteroidal anti-androgen bicalutamide acquires agonistic properties during long-term androgen ablation. These findings may have repercussions on the natural course of prostate cancer with androgen deprivation and on strategies of therapeutic intervention.  (+info)

Equilibrium in the hydrolysis and synthesis of cannabimimetic anandamide demonstrated by a purified enzyme. (6/409)

Anandamide, an endogenous ligand for cannabinoid receptors, loses its biological activities when it is hydrolyzed to arachidonic acid and ethanolamine by anandamide amidohydrolase. We overexpressed a recombinant rat enzyme with a hexahistidine tag in a baculovirus-insect cell expression system, and purified the enzyme with the aid of a Ni-charged resin to a specific activity as high as 5.7 micromol/min/mg protein. The purified recombinant enzyme catalyzed not only the hydrolysis of anandamide and palmitoylethanolamide, but also their reverse synthetic reactions. In order to attain an equilibrium of the anandamide hydrolysis and its reverse reaction within 10 min, we utilized a large amount of the purified enzyme. The equilibrium constant ([arachidonic acid][ethanolamine])/([anandamide][water]) was calculated as 4x10(-3) (37 degrees C, pH 9.0). These experimental results with a purified enzyme preparation quantitatively confirmed the reversibility of the enzyme reaction previously observed with crude enzyme preparations.  (+info)

Enzymes as reagents in peptide synthesis: enzymatic removal of amine protecting groups. (7/409)

A model system is described for the enzymatic deprotection of suitably masked amino groups during stepwise peptide synthesis. Nitrophenyl esters of amino acids, N-protected with trypsin-labile benzyloxycarbonylarginyl groups, were prepared as crystalline, analytically pure picrate salts in a standardized procedure. These intermediates were shown to react with amino compounds to form the expected peptide linkages. A pair of diasteriomeric peptides prepared in this way and featuring benzyloxycarbonylarginyl-L-, AND -D-glutaminyl sequences, respectively, were subjected to tryptic digestion. In both cases, a specific cleavage of the arginyl bond was achieved; however, the peptide containing the L-glutaminyl residue was deprotected much more rapidly than its diasteriomer containing the D-glutaminyl residue. The hydrolysis of the former isomer was not noticeably impeded by the presence of the latter. The results of these studies suggest that C-activated amino-acid derivatives, N-protected with trypsin-labile groups, are readily prepared in convenient form and that the peptide derivatives prepared from these intermediates are readily freed of their amino-protecting groups under mild, aqueous conditions with a potentially useful degree of stereospecificity. Theoretical implications of this first enzyme-catalyzed step in the repetitive cycle of peptide elaboration are discussed along with the procedural advantages implicit in the alternation of strongly and weakly basic groups in the protected and unprotected peptide intermediates, respectively.  (+info)

Bicalutamide monotherapy versus flutamide plus goserelin in prostate cancer patients: results of an Italian Prostate Cancer Project study. (8/409)

PURPOSE: To compare the efficacy of bicalutamide monotherapy to maximal androgen blockade (MAB) in the treatment of advanced prostatic cancer. PATIENTS AND METHODS: Previously untreated patients with histologically proven stage C or D disease (American Urological Association Staging System) were randomly allocated to receive either bicalutamide or MAB. After disease progression, patients treated with bicalutamide were assigned to castration. The primary end point for this trial was overall survival. Secondary end points included response to treatment, disease progression, treatment safety, quality-of-life (QOL), and sexual function. RESULTS: A total of 108 patients received bicalutamide and 112 received MAB. There was no difference in the percentage of patients whose prostate-specific antigen returned to normal levels. At the time of the present analysis (median follow-up time, 38 months; range, 1 to 60 months), 129 patients progressed and 89 died. There was no difference in the duration of either progression-free survival or overall survival. However, a survival trend favored bicalutamide in stage C disease but MAB in stage D disease. Overall and subgroup trends were confirmed by multivariate analysis. Serious adverse events and treatment discontinuations were more common in patients receiving MAB (P =.08 and P =.04, respectively). Fewer patients in the bicalutamide group complained of loss of libido (P =. 01) and of erectile dysfunction (P =.002). Significant trends favored bicalutamide-treated patients also with respect to their QOL, namely relative to social functioning, vitality, emotional well-being, and physical capacity. CONCLUSION: Bicalutamide monotherapy yielded comparable results relative to standard treatment with MAB, induced fewer side effects, and produced a better QOL.  (+info)

Tosyl compounds are organic compounds that contain the tosyl group (p-toluenesulfonyl, -SO2C6H4CH3) as a substituent. The tosyl group is a protecting group or a good leaving group in organic reactions. Tosyl compounds are often prepared by reacting alcohols or amines with p-toluenesulfonyl chloride (TsCl) in the presence of a base.

The general formula for a tosyl compound can be represented as R-OTs, where R represents an organic group such as an alkyl, aryl, or heteroaryl group. Tosyl compounds are widely used in organic synthesis due to their versatility and reactivity.

doi:10.1039/C2OB26253C (Functional groups, Hydrazones, P-Tosyl compounds). ... and Unsaturated Diazo Compounds and Its Application in Catalytic and Asymmetric Epoxidation of Carbonyl Compounds. Extensive ... Organic compounds having this functional group can be accessed by reaction of an aldehyde or ketone with tosylhydrazine. As an ... A tosylhydrazone in organic chemistry is a functional group with the general structure RR'C=N-NH-Ts where Ts is a tosyl group. ...
In general, acyl halides (even non-volatile compounds such as tosyl chloride) are irritants to the eyes, skin and mucous ... an alcohol to form an ester an amine to form an amide an aromatic compound, using a Lewis acid catalyst such as AlCl3, to form ... In organic chemistry, an acyl halide (also known as an acid halide) is a chemical compound derived from an oxoacid by replacing ... An important use of adipoyl chloride is polymerization with an organic di-amino compound to form a polyamide called nylon or ...
This group is usually derived from the compound tosyl chloride, CH3C6H4SO2Cl (abbreviated TsCl), which forms esters and amides ... Tosyl (Ts) group is commonly used as a protecting group for amines in organic synthesis. Tosyl chloride and pyridine in ... often through addition of tosyl chloride. In this reaction, the lone pair of the alcohol oxygen attacks the sulfur of the tosyl ... A tosyl group can function as a protecting group in organic synthesis. Alcohols can be converted to tosylate groups so that ...
Azido compounds, Reagents for organic chemistry, P-Tosyl compounds). ... Tosyl azide can be prepared by the reaction of tosyl chloride with sodium azide in aqueous acetone. Tosyl azide is one of the ... Tosyl azide is a reagent used in organic synthesis. Tosyl azide is used for the introduction of azide and diazo functional ... most stable azide compounds but is still regarded as a potential explosive and should be carefully stored, while particular ...
P-Tosyl compounds, All stub articles, Biochemistry stubs). ... Tosyl phenylalanyl chloromethyl ketone (TPCK) is a protease ...
P-Tosyl compounds, All stub articles, Gastrointestinal system drug stubs). ...
P-Tosyl compounds, Butyl compounds). ... Development of these compounds was taken over by German ... specifically from attempts to develop sulfa compounds. One of the contenders for a new sulfa antibiotic had serious side ...
P-Tosyl compounds, Sulfonamides, All stub articles, Sedative stubs). ... ROD-188 is one of a number of related compounds acting at this novel modulatory site, some of which also act at benzodiazepine ... Sigel E, Baur R, Furtmueller R, Razet R, Dodd RH, Sieghart W (June 2001). "Differential cross talk of ROD compounds with the ...
... a tosyl compound OpenTimestamps, a cryptographic timestamping standard Orthodox Theological Seminary, Kottayam, a seminary ...
P-Tosyl compounds, Nitrogen-halogen compounds, Sulfur-nitrogen compounds). ... Chloramine-T is the organic compound with the formula CH3C6H4SO2NClNa. Both the anhydrous salt and its trihydrate are known. ... Chemical articles with multiple compound IDs, Multiple chemicals in an infobox that need indexing, Chemical articles with ...
Pyridinium compounds, Salts, Reagents for organic chemistry, P-Tosyl compounds). ...
P-Tosyl compounds, All stub articles, Gastrointestinal system drug stubs). ...
Organoboron compounds, Sulfonamides, P-Tosyl compounds, All stub articles, Organic compound stubs). ... Diazaborine B is a chemical compound that inhibits maturation of rRNAs for the large ribosomal subunit. Pertschy, B.; Zisser, G ...
P-Tosyl compounds). ... Tosyl Collidinium p-toluenesulfonate Merck Index, 11th Edition ... The CH3C6H4SO2 group is known as the tosyl group and is often abbreviated as Ts or Tos. Most often, TsOH refers to the ... p-Toluenesulfonic acid (PTSA, pTSA, or pTsOH) or tosylic acid (TsOH) is an organic compound with the formula CH3C6H4SO3H. It is ... Chemical articles with multiple compound IDs, Multiple chemicals in an infobox that need indexing, Chemical articles with ...
The reaction of this imine with TsCl in pyridine to the ring-closed N-tosyl compound 8 was described by Woodward as a concerted ... This compound should form as a diastereomeric pair but only one compound was found although which one was not investigated. ... In this effort one of strychnine's many degradation products was synthesised first (the relay compound), a compound also ... In it N-tosyl amine 1 reacted with allyl carbonate 2 in an allylic asymmetric substitution using Pd2(dba)3 and asymmetric ...
P-Tosyl compounds). ... is an organic compound with the formula CH3C6H4SO2CH2NC. The ...
P-Tosyl compounds, Foul-smelling chemicals). ... The preparation of tosyl esters and amides are conducted in the ... HCl Tosyl chloride is considered to be a toxic and corrosive substance. "P-TOLUENESULFONYL CHLORIDE (TOSYL CHLORIDE)". Whitaker ... 4-Toluenesulfonyl chloride (p-toluenesulfonyl chloride, toluene-p-sulfonyl chloride) is an organic compound with the formula ... In characteristic manner, TsCl converts alcohols (abbreviated ROH) into the corresponding toluenesulfonate esters, or tosyl ...
P-Tosyl compounds). ... the Fate of Foreign Compounds in Biological Systems. 25 (12): ... "Divergent cardiac effects of the first and second generation hypoglycemic sulfonylurea compounds". Diabetes Research and ...
DPPA is very toxic and a potential explosive like most other azide compounds. Tosyl azide Trifluoromethanesulfonyl azide ... Azido compounds, Reagents for organic chemistry, Phenol esters, Phenyl compounds). ... Diphenylphosphoryl azide (DPPA) is an organic compound. It is widely used as a reagent in the synthesis of other organic ... This compound is used as a reagent for the synthesis of peptides by virtue of its reactions with carboxylic acids leading to ...
... formed using tosyl chloride). Hence this three reaction sequence provides three spiro compounds (ketone, alcohol, and alkane), ... spiro compounds are compounds that have at least two molecular rings with only one common atom. The simplest spiro compounds ... and chemical properties associated with aromatic compounds are still observed for such compounds. A spiro compound, or spirane ... For example, compound A in the image is called 1-bromo-3-chlorospiro[4.5]decan-7-ol, and compound B is called 1-bromo-3- ...
... tosyl compounds MeSH D02.886.590.887.140 - bromcresol green MeSH D02.886.590.887.150 - bromcresol purple MeSH D02.886.590.887. ... trialkyltin compounds MeSH D02.691.850.900.910 - triethyltin compounds MeSH D02.691.850.900.950 - trimethyltin compounds MeSH ... tosyl compounds MeSH D02.455.426.559.389.832.670 - tosylarginine methyl ester MeSH D02.455.426.559.389.832.690 - tosyllysine ... mustard compounds MeSH D02.455.526.728.468 - mustard gas MeSH D02.455.526.728.650 - nitrogen mustard compounds MeSH D02.455. ...
This compound serves as a building block for macrocyclizations. Many kinds of aza crown ethers exist. Variable length linkers ... By reaction with tosyl chloride, diethylene triamine is converted to a derivative with two secondary sulfonamides. ... "Proton coordination by polyamine compounds in aqueous solution". Coordination Chemistry Reviews. 188: 97-156. doi:10.1016/S0010 ...
Similar N-protected compounds such as N-t-BOC-methamphetamine, N-p-tosyl-methamphetamine, N-t-BOC-ketamine, N-t-BOC-norketamine ... N-t-BOC-MDMA is a chemical compound which can be both a synthetic precursor to, or a prodrug of the empathogenic drug MDMA. It ... Collins M, Bhattarai A, Salouros H (2018). "Another chemically masked drug: p‐tosyl methylamphetamine". Drug Testing and ...
In conjunction with aldehydes and ketones, tosyl isocyanides can be used to form α-hydroxy ketones after hydrolysis of the ... A variety of reagents exist to oxidize enolates to α-hydroxy carbonyl compounds-in the example here, oxy-Cope rearrangement ... Synthesis of α-hydroxy carbonyl compounds is most commonly accomplished by either chain extension or oxidation of carbonyl ... 9) Ketol isomerizations of secondary α-hydroxy carbonyl compounds, which proceed via tautomerization, are probably the closest ...
This compound is unstable (although not as much as [1.1.1]propellane; however it is less persistent than [1.1.1]propellane). ... and reaction with tosyl azide. The ketone then undergoes Wolff rearrangement to ketene 6. Ozonolysis forms the ketone 7, ... 2.2.2]Propellane, formally tricyclo[2.2.2.01,4]octane is an organic compound, a member of the propellane family. It is a ... This compound is converted to the diazo ketone 5 by deprotonation (using acetic acid and sodium methoxide) ...
Carbonyl compounds can also be coupled with simple alkenes to form five, six or eight membered rings. Tosyl groups can be ... Samarium(II) iodide is an inorganic compound with the formula SmI2. When employed as a solution for organic synthesis, it is ... Furthermore, hydrodehalogenation of halogenated hydrocarbons to the corresponding hydrocarbon compound can be achieved using ... Samarium compounds, Lanthanide halides, One-electron reducing agents, Reagents for organic chemistry). ...
Slow addition of the hydrazone is not necessary and it was found that this procedure is better suited for carbonyl compounds ... When strongly basic hydride donors are used such as lithium aluminium hydride, then deprotonation of the tosyl hydrazone can ... Several of the presented procedures require isolation of the hydrazone compound prior to reduction. This can be complicated by ... The reactions of hydrazones and related compounds with strong bases. Part I. A modified Wolff?Kishner procedure". Journal of ...
Chemistry of Heterocyclic Compounds: A Series Of Monographs. New York, USA: John Wiley & Sons, Inc. doi:10.1002/0471221902. ... Another azide regular is tosyl azide here in reaction with norbornadiene in a nitrogen insertion reaction: Some azides are ... The azo-transfer compounds, trifluoromethanesulfonyl azide and imidazole-1-sulfonyl azide react with amines to give the ... On a new class of compounds in which nitrogen is substituted for hydrogen". Proceedings of the Royal Society of London. 13: 375 ...
... is a macrocyclic compound and a bicyclam derivative, the cyclam rings being linked at the amine nitrogen atoms by a ... Three of the four nitrogen atoms of the macrocycle cyclam... (1,4,8,11-tetraazacyclotetradecane) are protected with tosyl ... After cleaving of the tosyl groups with hydrobromic acid, plerixafor octahydrobromide is obtained. The molecule was first ... synthesised in 1987 to carry out basic studies on the redox chemistry of dimetallic coordination compounds. Then, it was ...
Tosyl Compounds * chloramine-T * Tetraethylammonium * 4-Aminopyridine * Potassium Grants and funding * NS-17510/NS/NINDS NIH ...
doi:10.1039/C2OB26253C (Functional groups, Hydrazones, P-Tosyl compounds). ... and Unsaturated Diazo Compounds and Its Application in Catalytic and Asymmetric Epoxidation of Carbonyl Compounds. Extensive ... Organic compounds having this functional group can be accessed by reaction of an aldehyde or ketone with tosylhydrazine. As an ... A tosylhydrazone in organic chemistry is a functional group with the general structure RRC=N-NH-Ts where Ts is a tosyl group. ...
6-[(p-tosyl)amino]hexanoic acid, compound with 2,2,2-nitrilotriethanol (1:1). ...
... binding compounds using the comparative molecular similarity indices analysis (CoMSIA) method. The compound set contained 67 ... binding compounds using the comparative molecular similarity indices analysis (CoMSIA) method. The compound set contained 67 ... Docking was used to identify the preferred binding modes for the nonsteroidal compounds within the AR ligand-binding pocket ( ...
Categories: Tosyl Compounds Image Types: Photo, Illustrations, Video, Color, Black&White, PublicDomain, CopyrightRestricted 1 ...
Compounds A5, A10, A20 and the reference compound N-tosyl-D-prolinecysteamine (TPC) (Appendix 2-figure 1) were selected through ... Design of compounds F (upper panel).. Synthesis of compound F1 (bottom panel). (i): CH2Cl2/pyridine/DMAP, RT; (ii): THF/LiOH 2 ... A) Representation of S and R isomers of compound E7 obtained with (B) Structural modification of compound B12. The changes in ... From hits to dimer-destabilizing compounds.. (A) Structures of the compounds identified in MS studies (in red the fragments ...
Raw data for new compounds described in the paper: "Remote Nucleophilic Allylation by Allylrhodium Chain Walking" Lam, Hon Wai ... "Synthesis of multisubstituted pyrroles by nickel-catalyzed arylative cyclizations of N-tosyl alkynamides" Lam, Hon Wai ( ... Raw data for new compounds described in the paper "Iridium-catalyzed 1,5-(aryl)aminomethylation of 1,3-enynes by alkenyl-to- ... Raw data for new compounds described in the paper "Iridium-catalyzed 1,5-(aryl)aminomethylation of 1,3-enynes by alkenyl-to- ...
Interference of sulfhydryl compounds with the inhibitory effect of N-tosyl-L-phenylalanylchloromethane on elongation factor Tu ... Compounds inhibiting the degradation of uracil in the fluid and in cells of ehrlich ascites tumour. 1965, Vol. 30, Issue 5, pp ... Oligonucleotidic compounds. XXXIV. Preparation of some β-L-ribonucleosides, their 2(3)-phosphates and 2,3-cyclic phosphates ... Oligonucleotidic compounds. XII. Synthesis of cytidylyl-(3→5)-cytidylyl-(3→5)-adenosine (CpCpA), an acceptor sequence of ...
Tosyl Compounds. Quinolones. Chelating Agents. Fluorescent Dyes. Microscopy, Fluorescence. Female. Male. Rights: © CSIRO 1996. ...
Morpholinium, 4-(2-((cyclohexylcarbonimidoyl)amino)ethyl)-4- ... Carbodiimides (1974). Morpholines (1974). Tosyl Compounds ( ... Compounds formed by the joining of smaller, usually repeating, units linked by covalent bonds. These compounds often form large ... Organic compounds containing the carboxy group (-COOH). This group of compounds includes amino acids and fatty acids. ... Morpholinium, 4-(2-((cyclohexylcarbonimidoyl)amino)ethyl)-4- ... Carbodiimides (1974). Morpholines (1974). Tosyl Compounds ( ...
N-alpha-Tosyl-L-lysine chloromethyl ketone hydrochloride exhibits an inhibitory effect on IFN-γ activities. ... N-alpha-Tosyl-L-lysine chloromethyl ketone hydrochloride is an inhibitor of trypsin-like protease. ... Drug-like Compound Libraries Compound Libraries for HTS/HCS Fragment Libraries General Fragment Libraries Characteristic ... N-alpha-Tosyl-L-lysine chloromethyl ketone hydrochloride is an inhibitor of trypsin-like Protease. N-alpha-Tosyl-L-lysine ...
1R2R)-(-)-N-p-Tosyl-12-diphenylethylenediamine 98 , High Purity Chemical Compound , CAS Number: 144222-34-4. $ 0.00 ...
Anilides, Autophagy, Cell Line, Tumor, Humans, Male, Nitriles, Taxoids, Tosyl Compounds. © 2023 Nuffield Department of Surgical ...
The compound tosyl-phenylalaninechloromethyl ketone (TPCK, below) is an affinity ligand for chymotrypsin. ...
The ring-opened products 3 may efficiently be converted to homochiral 2-tosylaminocarbonyl compounds 4. ... Osborn, Helen M.I. and Sweeney, J. B. and Howson, Bill (1993) Ring-opening of N-tosyl aziridines by sulphur-stabilized ...
In the title N-tosyl-acryl-amide compounds, C20H17NO4S, (I), and C23H21NO3S, (II), the conformation about the C=C bond is E. ... Crystal structures of (E)-3-(furan-2-yl)-2-phenyl-N-tosyl-acryl-amide and (E)-3-phenyl-2-(m-tol-yl)-N-tosyl-acryl-amide. ... There is an intra-molecular C-Hâ ¯π inter-action present in compound (II). In the crystals of both compounds, mol-ecules are ... The compound crystallizes in the monoclinic space group I2/a. In the mol-ecule, the four rings are not in the same plane, the ...
Small quantities of tosyl azide were accessed in a one pot batch procedure using shelf stable, readily available reagents. ... The in situ formed tosyl azide was used to rapidly perform diazo transfer to a range of acceptors, including beta-ketoesters, ... For large scale diazo transfer reactions tosyl azide was generated and used in a telescoped flow process, to mitigate the risks ... Heat and shock sensitive tosyl azide was generated and used on demand in a telescoped diazo transfer process. ...
The title compound, (I). , is similar to the macrocycle reported by Halfpenny & Sloman (2000. ), in that the bulky tosyl ... The title compound, C34H42N2O9S4, is composed of two thio-phene rings bridged by an -O-(CH2)2-O-(CH2)2-O- chain and a tri- ... C14 and the longest between the two tosyl rings is 9.983 (3) Å for C25⋯C29. The large separation of the two tosyl rings ... Compound (I). was synthesized according to the procedure described by Chaffin et al. (2002. ). Crystals suitable for X-ray ...
Preferred W leaving groups in the compound of formula XIV include tosyl, mesyl, chloro, bromo, iodo, and ... The compounds of formula XII are either known compounds or are prepared from known compounds by conventional processes for ... e) treatment of compound XVII with a nonnucleophilic strong base to form a compound of formula IX(a) which is tautomeric with ... Step (g), is wherein the reaction of compounds of formulas IX(a) and IX(b) with compounds of formula XII is conducted in an ...
Tosyl Isocyanate is the synthetic and aromatic silane compound with an isocyanate group, that confroms to the formula: C8 ... Tosyl Isocyanate. Tosyl Isocyanate is the synthetic and aromatic silane compound with an isocyanate group, that confroms to the ...
Structures of compounds were elucidated by analysis of their 1H and 13C NMR spectra, MS spectra and elemental analyses. N-7 ... In this report, we describe alternative success in the deprotection of N-tosyl-animopyrazine triflate before the cross coupling ... Compound (3) showed moderate cytotoxic activity against HSC-2 human squamous cell carcinoma cells with an IC50 value of 16 μg/ ... This compound enables us to synthesize various coelenterazine analogs. This triflate was proven to be so important intermediate ...
Gabexate mesylate, N-p-Tosyl-Gly-Pro-Arg p-nitroanilide acetate salt, tryptase from the human lung, compound 48/80, sodium ... The compound 48/80 leads to the degranulation of mast cells, promoting the release of mediators such as histamine, serotonin, ... Compound 48/80, that promotes depletion of mast cell mediators, was administered daily at increasing doses (1, 3, 10, and 10 µg ... The effect of pretreatment for 4 days (1+ 3+ 10+ 10 µg/paw, intraplantar [i.pl.]) with compound 48/80 on tryptase activity in ...
Three new kinds of analogous compounds, C6H11NH2HN(SO3HC6H11NH2)2, C6H11NH2-HN(SO3Na)2, and C6H11NH2HN(SO3)2Ca, were prepared ... Since the rearrangement of quinoline 1-oxide with tosyl chloride results in variety of reactions, it was important that the ... tosyl derivative was obtained as an intermediate. Nitration of 5-methylcarbostyril gave the 6-nitro compound and 5-methyl-6- ... All the compounds tested showed better antitubercular action than pyrazinamide used as the control but none had better ...
Compound of formula II can be converted into a facile leaving group by treating with tosyl chloride, methane sulfonyl chloride ... 7. A process as claimed in claim 6 wherein compound of formula II is. converted to compound of formula IX by reacting compound ... a) reacting compound of formula III with the anion of tertiary. butyl acetate to give a compound of formula IV, where G is. ... The compound of formula II is oxidized to a compound of formula VIII, where R3 is alkyl from 1 to 8 carbons, aryl or aralkyi ...
These new polyanionic compounds that contain multiple metallacarborane clusters at their periphery may prove useful as new ... These led to new terminal groups (chloro, bromo, and tosyl leaving groups, organic acid, and azide) that permitted ester ... Polyanionic species were obtained in high yield through the ring-opening reaction of cyclic oxonium compound [3,3′-Co(8-C4H8O2- ... classes of compounds for boron neutron capture therapy with enhanced water solubility and as cores to make a new class of high- ...
... from commercially available halogenated compounds. This method is a fast and environmentally-friendly tool in medicinal ... furyl and tosyl-containing substituents. ... from commercially available halogenated compounds. This method ...
After 30 minutes adsorption at room temperature, 2 mL/well minimal essential medium supplemented with 2 mg/mL tosyl ... Oseltamivir carboxylate, the active compound of the ethyl ester prodrug oseltamivir phosphate, was kindly provided by Hoffmann- ...
General procedure for acetylation of the lone hydroxy group in compounds 5 and 10: synthesis of compounds 6 and 11. To a ... The tosyl derivatives 5 and 10 of dihydroxyfuranosides 4a and 4b were obtained by their tosylation with TsCl-pyridine in 94 and ... General procedure for the acetolysis of compounds 6 and 11: synthesis of tetraacetate compounds 7a,b and 12a,b. Similar as ... The structures of all the synthesized compounds, i.e., 4a, 4b, 5, 6, 7a,b, 8-11, 12a,b, 13 and 14 were unambiguously ...
... described the vitamin B12-photocatalyzed cyclization of N-tosyl amines carrying an ω-bromoalkyl and an allyl group, which ... and light as the source of energy can facilitate the synthesis of complex and valuable organic compounds, including ...
Tosyl esters have been made from alcohols and tosyl chlorides. However I shouldnt suggested a method of converting carboxylic ... It is different than sulphurous compounds or chlorine and very persistent.. TsCl is insoluble in water, so after diluting it ... The resulting cloudy liquid should contain tosyl chloride and was stored for next steps.. Maybe there was only sulphur ... Has anyone experience with acetonitril and tosyl esters (vanillin solubility seems adequate)?. Maybe trying a melt-phase ...
  • Using this powerful method it is possible to access bioactive compounds. (wikipedia.org)
  • link A New Protocol for the In Situ Generation of Aromatic, Heteroaromatic, and Unsaturated Diazo Compounds and Its Application in Catalytic and Asymmetric Epoxidation of Carbonyl Compounds. (wikipedia.org)
  • doi:10.1002/ejoc.200400700 Catalytic Cyclopropanation of Alkenes Using Diazo Compounds Generated in Situ. (wikipedia.org)
  • The in situ formed tosyl azide was used to rapidly perform diazo transfer to a range of acceptors, including beta-ketoesters, beta-ketoamides, malonate esters and beta-ketosulfones. (ucc.ie)
  • The invention also relates to methods of using antibodies and antibody-drug conjugate compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions. (justia.com)
  • c) protecting the compound of formula V with ArB(0H)2 to give a compound of formula VI, where Ar is unsubstituted or substituted aryl or heteroaryl, G is tetrahydropyranyl, tert-butyldimethyl silyl or trityl and R3 is alkyl from 1 to 8 carbons, ( f) deprotection of the compound of formula VI using mild acid catalyst to give a compound of formula II. (allindianpatents.com)
  • The compound of formula II is oxidized to a compound of formula VIII, where R3 is alkyl from 1 to 8 carbons, aryl or aralkyi and Ar is unsubstituted or substituted aryl or heteroaryl using pyridinium chioro chromate or DMSO/oxalyl chloride. (allindianpatents.com)
  • in that the bulky tosyl substituents may have a major effect on the macrocyclic ring geometry. (iucr.org)
  • The flexibility of the approach was demonstrated using a diversity of primary amines with benzyl, aromatic, aliphatic, furyl and tosyl-containing substituents. (eurekaselect.com)
  • Tosyl Isocyanate is the synthetic and aromatic silane compound with an isocyanate group, that confroms to the formula: C 8 H 7 NO 3 S. (productingredients.com)
  • Heat and shock sensitive tosyl azide was generated and used on demand in a telescoped diazo transfer process. (ucc.ie)
  • Small quantities of tosyl azide were accessed in a 'one pot' batch procedure using shelf stable, readily available reagents. (ucc.ie)
  • For large scale diazo transfer reactions tosyl azide was generated and used in a telescoped flow process, to mitigate the risks associated with handling potentially explosive reagents on scale. (ucc.ie)
  • These led to new terminal groups (chloro, bromo, and tosyl leaving groups, organic acid, and azide) that permitted ester production, click chemistry, and oxonium ring opening to be performed as examples of reactions that demonstrate the wide possibilities of the globular icosahedral carboranes to produce new dendritic or dendrimer-like structures. (icmab.es)
  • Polyanionic species were obtained in high yield through the ring-opening reaction of cyclic oxonium compound [3,3′-Co(8-C4H8O2-1,2-C2B9H10)(1′,2′-C2B9H11)] by using terminal hydroxyl groups as nucleophiles. (icmab.es)
  • Experimental and Theoretical Analysis of the Thiol-Promoted Fragmentation of 2-Halo-3-tosyl-oxanorbornadienes. (us.es)
  • The present invention relates to optically active dihydroxy hexanoate derivatives of formula IIa and more particularly to compounds of formula II which are useful intermediates for the synthesis of HMG-CoA enzyme inhibitors like atorvastatin, cerivastatin, rosuvastatin, pitavastatin, fluvastatin. (allindianpatents.com)
  • The synthesis of the ribo - trihydroxy sugar derivative starting from diacetone-D-glucose led to the formation of an inseparable 1:1 mixture of the required compound and its C-3 epimer, i.e., 4- C- hydroxymethyl-1,2- O -isopropylidene-α-D-xylofuranose [10] . (beilstein-journals.org)
  • Professor Gryko said: "We demonstrated that nature native cobalt complex - vitamin B12 - and light as the source of energy can facilitate the synthesis of complex and valuable organic compounds, including pyrrolidines and piperidines. (thieme.de)
  • Organic compounds having this functional group can be accessed by reaction of an aldehyde or ketone with tosylhydrazine. (wikipedia.org)
  • Hydrolysis is the reverse reaction of formation with regeneration of the carbonyl compound. (wikipedia.org)
  • Following a literature procedure, we synthesized gram amounts of 1 from N-tosyl aniline, Scheme 1.three Initial evaluation of the reaction in between ynesulfonamide 1 and benzoyl chloride showed that copper(I) salts have been superior more than each zinc and palladium complexes typically made use of in alkynylation reactions. (adenosine-receptor.com)
  • The Bischler-Napieralski reaction of N-(5-benzyloxy-3, 4-dimethoxyphenethyl)-3-(3-ethoxycarbonyl-4-methoxyphenyl) propionamide (XX) also gave a mixture of 3, 4-dihydroisoquinolines which was derived to the 1, 2, 3, 4-tetrahydroisoquinolines and separated into 8-hydroxy (XXIV) and 6-hydroxy (XXV) compounds. (go.jp)
  • The Mitsunobu Reaction allows the conversion of primary and secondary alcohols to esters, phenyl ethers, thioethers and various other compounds. (organic-chemistry.org)
  • The mol-ecular structure of the title compound, with displacement ellipsoids drawn at the 50% probability level. (iucr.org)
  • A tosylhydrazone in organic chemistry is a functional group with the general structure RR'C=N-NH-Ts where Ts is a tosyl group. (wikipedia.org)
  • EP 0 319 847 describes a process for the preparation of compounds of formula 1 starting from L-Malic acid. (allindianpatents.com)
  • We studied the three-dimensional quantitative structure-activity relationships (3D QSAR) of 70 structurally and functionally diverse androgen receptor (AR) binding compounds using the comparative molecular similarity indices analysis (CoMSIA) method. (nih.gov)
  • A compound used in molecular biology to digest some proteins and as a coupling reagent for phosphoroamidate or pyrophosphate internucleotide bonds in DNA duplexes. (lookformedical.com)
  • What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol? (targetmol.com)
  • Perhaps the etherifed poly(ethylene glycols) can be used as solvents for Grignard reactions since they are close analogs to ethyl ether, are known to coordinate well with metal ions, and are at the very least totally inert to Grignard compounds. (thevespiary.org)
  • The large separation of the two tosyl rings influences the geometry of the macrocyclic cavity by ensuring that the thio-phene rings and therefore the O and N atoms do not lie in the same plane. (iucr.org)
  • They are sweet-tasting compounds that are used as chemical intermediates and plant growth stimulants. (lookformedical.com)
  • The computational chemistry in combination with mass spectrometry allows comprises several chemical events which may occur during the ionization and dissociation of a particular compound, through appropriated descriptors, for instance, gas-phase basicity, proton affinities, electron affinities and proton transfers. (fapesp.br)
  • Organic compounds containing the carboxy group (-COOH). (lookformedical.com)
  • Recently, the group of Professor Dorota Gryko (Polish Academy of Sciences, Warsaw, Poland) described the vitamin B12-photocatalyzed cyclization of N -tosyl amines carrying an ω-bromoalkyl and an allyl group, which occurs with subsequent C- dicarbofunctionalization in the presence of acrylic acid derivatives or acrylonitrile, leading to the corresponding cyclic amines. (thieme.de)
  • Mol-ecules of the title compound, C 15 H 16 O 5 S, are composed of a 3,5-di-meth-oxy-phenyl moiety substituted with a toluene-4-sulfonate group. (iucr.org)
  • The title compound, C 34 H 42 N 2 O 9 S 4 , is composed of two thio-phene rings bridged by an -O-(CH 2 ) 2 -O-(CH 2 ) 2 -O- chain and a tri-substitued diamine with pendent tosyl rings. (iucr.org)
  • In the asymmetric unit of the title compound there is one independent mol-ecule. (iucr.org)
  • The crystal packing of the title compound, viewed along the c axis. (iucr.org)
  • The title compound was placed in small portions until a saturated solution was obtained. (iucr.org)
  • N-alpha-Tosyl-L-lysine chloromethyl ketone hydrochloride (50 μM) exhibits a small decrease in cell viability. (targetmol.com)
  • It can modify a variety of drugs, such as protein drugs, peptide compounds, organic small molecule drugs and so on. (bocsci.com)
  • Nevertheless, the results will be combined with pka values obtained from computational methods in order to suggest the reactivity of compounds in solution. (fapesp.br)
  • The disadvantages of this process are that a stereo selective reduction using a costly ruthenium-BINAP catalyst in employed and the desired compound of formula 1 is obtained in six steps. (allindianpatents.com)
  • The 3.4-dihvdroxv hutanoir arid derivative is then functionalized into compounds of formula I involving a multiple number of steps. (allindianpatents.com)
  • With both receptors present in the same cell, the selectivity or nonselectivity of a variety of compounds that would affect PAR 1 and/or PAR 2 could be efficiently evaluated in a single experiment. (aspetjournals.org)
  • The Grignard reacts with the most availible substance, which is usually the starting compound, and not wit the end product. (thevespiary.org)