TY - JOUR. T1 - Asymmetric hydroformylation of styrene using rhodium and platinum complexes of diphosphites containing chiral chelate backbones and chiral 1,3,2-dioxaphosphorinane moieties. AU - Cserépi-Szucs, Stefánia. AU - Tóth, Imre. AU - Párkányi, László. AU - Bakos, József. PY - 1998/9/4. Y1 - 1998/9/4. N2 - Several chiral diphosphite ligands containing six stereogenic centres were synthesised and tested in order to study chiral cooperativity in the Rh- and Pt-catalysed asymmetric hydroformylation of styrene. The ligands were prepared either by the reaction of 2,4-pentanediol enantiomers with (4R,6R)- 4,6-dimethyl-2-chloro-1,3,2-dioxaphosphorinane or that of (1S,3S)-1,3- diphenyl-1,3-propanediol with 4,6-dimethyl-2-chloro-1,3,2-dioxaphosphorinane enantiomers. Thus the chirality was varied both in the chelate backbone and in the terminal groups of the ligands. In case of Pt-catalysed hydroformulation, the stereogenic elements in the bridge have been found to be determinate for the ...

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The invention provides a novel method for the chemical synthesis of 2′,3′-cyclic phosphate and phosphorothioate of mono and terminated oligonucleotides synthesis. The invention also provides a novel method of for the chemical synthesis of 2′,3′- and 3′,5′-cyclic phosphate and phosphorothioate mononucleotide nucleotides. The process is based on quick and efficient cyclization of phosphoramidate moiety and neighboring hydroxyl group. The present invention is directed towards the synthesis of high purity DNA and RNAs, specifically to introduce cyclic phosphate at 3′-end of oligonucleotides. Such DNA and RNAs have extensive application in therapeutics, diagnostics, drug design, and selective inhibition of an RNA sequence within cellular environment, in pre-tRNA cleavage and in ribozyme ligation. The 2′,3′-cyclic phosphate nucleosides are involved in a vast number of applications in molecular biology in general and mammalian cells in particular. The invention also envisions providing kits

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This thesis describes the synthesis and radiohalogenation of compounds of potential use for tumor targeting.. The first section describes the synthesis and radioiodination of DNA intercalating compounds. The compounds are derivatives of 9-aminoacridine, and the anthracyclins daunorubicin and doxorubicin. The precursor compounds were labeled with 125I (T1/2 = 60 days), which is an Auger emitting nuclide. 125I decaying in the close vicinity of DNA is known to have a much higher cell killing effect than 125I decaying in the cytoplasm and some of the labeled compounds prepared in this thesis are currently being tested for use in targeted radionuclide therapy for cancer.. The second section describes the radiobromination of closo-carboranes by subjecting the corresponding iodinated compounds to palladium-catalyzed halogen exchange using [76Br]bromide. The 76Br isotope (T1/2 = 16.2 h) is a positron emitting nuclide that is suitable for PET studies. Via the halogen exchange reaction good to excellent ...

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To overcome this issue of reduced resolution in STED imaging due to photodegradation, ITbMs team led by Principal Investigators Shigehiro Yamaguchi, a synthetic chemist and Tetsuya Higashiyama, a plant biologist have developed a new fluorescent dye, C-Naphox that has enhanced photostability relative to conventional dyes. C-Naphox has demonstrated to be extremely photoresistant with almost no degradation of fluorescence even after prolonged STED imaging in live cells.. C-Naphox (diarylmethylene-bridged naphthophosphole P-oxide) consists of an aromatic framework with an amino moiety incorporated for its electron-donating properties and phosphorus oxide for its electron-accepting properties, leading to intense fluorescence emissions.. Although the previously synthesized molecules in the Yamaguchi group have also led to high fluorescence intensity, it is the carbon-bridged structure in C-Naphox that is the key to its extremely high resistance to high intensity light, says Aiko Fukazawa, an ...

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Bartl, Joerg; Steenken, S.; Mayr, Herbert und McClelland, R. A. (1990): Photo-heterolysis and -homolysis of substituted diphenylmethyl halides, acetates, and phenyl ethers in acetonitrile: characterization of diphenylmethyl cations and radicals generated by 248-nm laser flash photolysis. In: Journal of the American Chemical Society, Vol. 112, Nr. 19: S. 6918-6928 ...

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Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice. ...

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Cyclic phosphatidic acid (cPA) has an inhibitory effect on the autotaxin (ATX)/lysophosphatidic acid (LPA) axis, which has been implicated to play an important role in the progression of fibrosis in systemic sclerosis (SSc). The purpose of this study is to assess the antifibrotic activity of cPA for the treatment of SSc using SSc skin fibroblasts and an animal model of bleomycin-induced skin fibrosis. We used a chemically stable derivative of cPA (2ccPA). First, we investigated the effect of 2ccPA on extracellular matrix (ECM) expression in skin fibroblasts. Next, the effect of 2ccPA on the intracellular cAMP levels was determined to investigate the mechanisms of the antifibrotic activity of 2ccPA. Finally, we administered 2ccPA to bleomycin-induced SSc model mice to evaluate whether 2ccPA prevented the progression of skin fibrosis. 2ccPA decreased ECM expression in SSc skin fibroblasts and TGF-β1-treated healthy skin fibroblasts without LPA stimulation. 2ccPA increased the intracellular cAMP levels in

TY - JOUR. T1 - ATR inhibition broadly sensitizes ovarian cancer cells to chemotherapy independent of BRCA status. AU - Huntoon, Catherine J.. AU - Flatten, Karen S.. AU - Wahner Hendrickson, Andrea E.. AU - Huehls, Amelia M.. AU - Sutor, Shari L.. AU - Kaufmann, Scott H.. AU - Karnitz, Larry M.. PY - 2013/6/15. Y1 - 2013/6/15. N2 - Replication stress and DNA damage activate the ATR-Chk1 checkpoint signaling pathway that licenses repair and cell survival processes. In this study, we examined the respective roles of the ATR and Chk1 kinases in ovarian cancer cells using genetic and pharmacologic inhibitors in combination with cisplatin, topotecan, gemcitabine, and the PARP inhibitor veliparib (ABT-888), four agents with clinical activity in ovarian cancer. RNA interference (RNAi)-mediated depletion or inhibition of ATR sensitized ovarian cancer cells to all four agents. In contrast, while cisplatin, topotecan, and gemcitabine each activated Chk1, RNAi-mediated depletion or inhibition of this ...

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On the basis of the preclinical and clinical studies, 1592U89 appears to be a promising agent for treatment of HIV infection in children, either as an alternative to currently employed agents, or in combination therapy regimens. A liquid formulation of the drug is available; thus concurrent development of 1592U89 for children and adults is possible.. In part 1, patients will receive 1592U89 monotherapy for 12 weeks. Patients will be assigned initially to a low dose of 1592U89 (Dose A). Those patients who tolerate the drug for at least six weeks without a toxicity of grade 3 or above attributable to study drug will have their 1592U89 dose increased (Dose B). If none of those patients experience a life threatening event attributable to study drug, subsequent enrollees will be assigned initially to Dose B. In part 2, each participant will be assigned randomly (1:1:1:1) within their age and Part 1 regimen stratum to one of the four agents: Zidovudine (ZDV), Stavudine (d4T), Didanosine (ddI) or ...

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These enzymes form some of the cyclic phosphate Ins(cyclic1,2)P(4,5)P2 as well as Ins(1,4,5)P3. They show activity towards phosphatidylinositol, i.e., the activity of EC 4.6.1.13, phosphatidylinositol diacylglycerol-lyase, in vitro at high [Ca2+]. Four beta-isoforms regulated by G-proteins, two gamma-forms regulated by tyrosine kinases, four delta-forms regulated at least in part by calcium and an epsilon-form, probably regulated by the oncogene ras, have been found ...

The design and total synthesis of DL-6-deoxy-6-(hydroxymethyl)-scyllo-inositol 1:7-cyclic 2,4-trisphosphate (4), a conformationally restricted cyclic phosphate analogue of the second messenger inositol 1,4,5-trisphosphate [Ins(1,4,5)P 3 ], is described. The protected inosose 2,4,6/3,5-pentahydroxy-3,5-bis-O-(p-methoxybenzyl)-2,4,6-O- methylidynecyclohexanone (7) was obtained from myoinositol orthoformate in two steps, and Wittig methylenation and then hydroboration-oxidation using 9-BBN-H/OH - /H 2 O 2 gave the axial hydroxymethyl derivative 9. A series of protection/ deprotection steps provided the diol 13, which was converted into two cyclic phosphate esters 14a and 14b, epimeric at phosphorus, by reaction with (benzyloxy)bis(N,N-diisopropylamino)phosphine/ 1H-tetrazole followed by m-CPBA. Two other hydroxyl groups were then exposed and phosphorylated, and total deprotection gave racemic 4. NMR studies confirmed that in 4 the phosphate group equivalent to the 4-phosphate of Ins(1,4,5)P 3 is held in

S-Alkylation of 5-(diphenylmethyl)-1,3,4-oxadiazole-2(3H)-thione (3) by 2-chloro-N-(pyrazin-2-yl)acetamide (2) affords the title compound, 2-{[5-(diphenylmethyl)-1,3,4-oxadiazol-2-yl]sulfanyl}-N-(pyrazin-2-yl)acetamide (4). The intermediate (2), in turn, was prepared by the acetylation of 2-aminopyrazine (1) with chloroacetyl chloride. The structure of the newly synthesized compound is characterized by IR, NMR and mass spectral data.

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Disclosed is a toothpaste binder composition comprising semi-refined carrageenan. Examples of semi-refined carrageenan suitable for incorporation into a toothpaste binder are semi-refined kappa carrageenan and semi-refined iota carrageenan. Such a toothpaste binder may comprise, for example, semi-refined kappa carrageenan, semi-refined iota carrageenan, or a combination of both semi-refined kappa and iota carrageenan. Such a formulation is preferably comprised of about 10% to about 20% refined kappa-2/lambda carrageenan; about 35% to about 50% refined iota carrageenan; about 20% to about 30% semi-refined kappa and/or semi-refined iota carrageenan; and about 5% to about 20% standardizing agent; by dry weight. Specific formulations incorporating semi-refined carrageenan are described. Properties and characteristics exhibited by a toothpaste which incorporates the specific binder formulations are also described. Also disclosed is a toothpaste binder composition comprising a semi-refined carrageenan, such

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Flow Properties of Lambda Carrageenan in Aqueous Systems. By Andrea Rivera del Rio, Mariana Ramírez-Gilly and Alberto Tecante. Small amplitude oscillatory and steady shear measurements at 25°C were used to investigate the rheological behavior of λ‐carrageenan solutions at pH 7.0 ± 1.0 without and with added sodium counterion. The dynamic moduli, G′(ω) and G″(ω), show the typical behavior of macromolecular solutions in which the viscous character predominates. The steady shear flow exhibits a Newtonian zero‐shear viscosity (η0) region followed by a shear‐thinning zone. Viscosity data can be well described by the Carreau‐Yasuda model. Without added Na+, the intrinsic viscosity, [η], and the critical overlap concentration, C*, are 204 dL/g and 0.21%, respectively. With 20 mmol/dm3 Na+, [η] = 14.7 dL/g and C* = 0.38%. For concentrations below C*, the viscous character is more sensitive to the presence of added Na+, and the opposite occurs when the concentration exceeds C*. The ...