- COMPOUNDS FOR THE REDUCTION OF THE DELETERIOUS ACTIVITY OF EXTENDED NUCLEOTIDE REPEAT CONTAINING GENES
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Aspects of the present disclosure include methods of reducing the deleterious impact of a target gene in a cell, such as the deleterious activity of a mutant extended nucleotide repeat (NR) containing target gene in a cell by contacting the cell with an effective amount of a tetrahydrocarbazole compound. The deleterious activity (e.g., toxicity and/or dis-functionality of products encoded thereby) of a mutant extended NR containing target gene may be reduced, e.g., by reducing (and in some instances differentially, including selectively, reducing) the production or activity of toxic expression products (e.g., RNA or protein) encoded by the target gene. Kits and compositions for practicing the subject methods are also provided.
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Page/Page column 62; 79
(2020/07/14)
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- Preparation and reactivity of polystyrene-supported iodosylbenzene: Convenient recyclable oxidizing reagent and catalyst
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A facile preparation of novel polystyrene-supported iodosylbenzene (PS-ISB, loading of IO up to 1.50 mmol/g) from iodopolystyrene is described. This resin has been successfully used for efficient oxidation of a diverse collection of alcohols to aldehydes and ketones in the presence of BF3OEt 2. PS-ISB can also be employed as efficient co-catalyst in combination with RuCl3 in the catalytic oxidation of alcohols and aromatic hydrocarbons, respectively, to corresponding carboxylic acids and ketones using Oxone as the stoichiometric oxidant. Georg Thieme Verlag Stuttgart ? New York.
- Chen, Jiang-Min,Zeng, Xiao-Mei,Middleton, Kyle,Yusubov, Mekhman S.,Zhdankin, Viktor V.
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experimental part
p. 1613 - 1617
(2011/08/03)
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- Efficient synthesis of cryptophycin-52 and novel para- Alkoxymethyl unit A analogues
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Cryptophycins are a family of highly cytotoxic, cyclic depsipeptides. They display antitumour activity that is largely maintained for multidrug-resistant tumour cells. Cryptophycins are composed of four building blocks (units A-D) that correspond to the respective amino and hydroxy acids. A new synthetic route to unit A allows the selective generation of all four stereogenic centres in a short, efficient and reliable synthesis and con-tributes to an easier and faster synthesis of cryptophycins. The first two stereogenic centres are introduced by a catalytic asymmetric dihydroxylation, whereas the remaining two stereogenic centres are introduced with substrate control of diastereoselectivity. The stereogenic diol function also serves as the epoxide precursor. The approach was used to synthesise the native unit A building block as well as three paraalkoxymethyl analogues from which cryptophycin-52 and three analogous cryptophycins were prepared. Macrocyclisation of the seco-depsipeptides was based on ring-closing metathesis.
- Eissler, Stefan,Bogner, Tobias,Nahrwold, Markus,Sewald, Norbert
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scheme or table
p. 11273 - 11287
(2010/04/28)
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- PYRROLOPYRIMIDIN-7-ONE DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
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Compounds of formula (I) or pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4, and R5 and are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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- Synthetic protocols and building blocks for molecular electronics
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Simple and readily accessible aryl bromides are useful building blocks for thiol end-capped molecular wires. Thus, 4-bromophenyl tert-butyl sulfide and 1-bromo-4-(methoxymethyl)benzene serve as precursors for a variety of oligo(phenylenevinylene) and olig
- Stuhr-Hansen, Nicolai,S?rensen, Jakob Kryger,Moth-Poulsen, Kasper,Christensen, J?rn Bolstad,Bj?rnholm, Thomas,Nielsen, Mogens Br?ndsted
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p. 12288 - 12295
(2007/10/03)
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- Oxidation of benzylic alcohols and ethers to carbonyl derivatives by nitric acid in dichloromethane
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Nitric acid in dichloromethane may be successfully employed for the oxidation of benzylic alcohols and ethers to the corresponding carbonyl compounds. The proposed method proved to be of general applicability, affording very good yields of aldehydes and ketones and showing interesting chemoselectivity in many instances, allowing competitive aromatic nitration to be avoided, as well as - in the case of aldehydes - any further oxidation to carboxylic acids. The reaction probably proceeds by a radical mechanism, the active species in the oxidation process being NO2. Competitive formation of nitro esters was observed in some cases, whereas poor results were obtained with allylic and non-benzylic substrates. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003.
- Strazzolini, Paolo,Runcio, Antonio
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p. 526 - 536
(2007/10/03)
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- Compositions containing aromatic aldehydes and their use in treatments
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Disclosed are pharmaceutical and cosmetic compositions containing aromatic aldehyde compounds. Some of the disclosed compositions are useful as topical therapeutics for treating inflammatory dermatologic conditions. Some of the compositions are useful in transdermal and other systemic dose forms for treating other inflammatory conditions in mammals.
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- A New Approach for Oxygenation Using Nitric Oxide under the Influence of N-Hydroxyphthalimide
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An approach for partial oxygenation through a carbocation as an intermediate was successfully developed by using nitric oxide under the influence of N-hydroxyphthalimide. Thus, a variety of benzylic ethers were converted into the corresponding partially oxidized compounds, which are difficult to prepare by conventional methods, in high yields. For example, the reaction of phthalane with NO in the presence of a catalytic amount of NHPI at 60°C gave phthalaldehyde in 80% yield. The reaction was found to proceed through the formation of a hemiacetal, such as 1-hydroxyphthalane. In addition, 1,3-di-tert-butoxymethyl benzene afforded 1,3-benzenedicarbaldehyde in good yield. On the other hand, isochroman was converted into 1,1′-oxodiisochromane under these reaction conditions. The reaction of ethers with NO in the presence of a NHPI catalyst is thought to proceed via the formation of a carbocation as an intermediate. A possible reaction path was suggested.
- Eikawa, Masahiro,Sakaguchi, Satoshi,Ishii, Yasutaka
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p. 4676 - 4679
(2007/10/03)
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- Synthetic Study of Selective Benzylic Oxidation
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Oxidation of bisbenzyl ethers was studied using 2,3-dichloro-5,6-dicyanobenzoquinone (DDQ). Compared to other benzylic oxidations such as Kornblum type reaction of benzyl bromides or MnO2 oxidation of benzyl alcohols, DDQ oxidation offered advantages of being mild and highly selective to provide monoaldehyde products. We have explored factors which influence the course of the reaction and exemplified the synthetic value of the approach by preparing a number of aromatic intermediates (7-8, 15-25).
- Wang, Wuyi,Li, Tiechao,Attardo, Giorgio
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p. 6598 - 6602
(2007/10/03)
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- 2-Hydroxy-2,2-dimethylacetic acid ester derived heterobiaryl ethers containing 1,3,5-triazine substituents
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The 1,3,5-triazines 3 were obtained from methyl 4-formylbenzoate (4) in a multistep synthesis by first introducing the ester unit under Williamson conditions. Subsequently, the 1,3,5-triazine ring was synthesized by reaction of isocyanates with 1,3-diazadienes obtained from N-silylimines.
- Barluenga,Del Pozo,Olano
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p. 1529 - 1533
(2007/10/02)
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- Thiazolidinedione hypoglycemic agents
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Hypoglycemic thiazolidine-2,4-dione derivatives of the formula STR1 wherein the dotted line represents a bond or no bond; A and B are each independently CH or N, with the proviso that when A or B is N, the other is CH; X is S, SO, SO2, CH2, CHOH or CO; n is 0 or 1; Y is CHR1 or NR2, with the proviso that when n is 1 and Y is NR2, X is SO2 or CO; Z is CHR3, CH2 CH2, CH=CH, STR2 OCH2, SCH2, SOCH2 or SO2 CH2 ; R, R1, R2 and R3 are each independently hydrogen or methyl; and X1 and X2 are each independently hydrogen, methyl, trifluoromethyl, phenyl, benzyl, hydroxy, methoxy, phenoxy, benzyloxy, bromo, chloro or fluoro; a pharmaceutically-acceptable cationic salt thereof; or a pharmaceutically-acceptable acid addition salt thereof when A or B is N.
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- Oxidative Cleavage of Ethers by Metallic Nitrates Supported on Silica Gel
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Metallic nitrates supported on silica gel efficiently cleave and oxidize ethers to the corresponding aldehydes or ketones under mild conditions.Silica gel is essential for the efficient oxidation, and Cu(NO3)2 and Zn(NO3)2 are suitable for practical use.Overoxidation of the product aldehydes is not observed.In some cases alkyl nitrites are isolated in addition to the carbonyl compounds, and the decomposition of alkyl nitrites to the corresponding carbonyl compounds is promoted by the presence of metallic nitrates supported on silica gel.Mechanistic study suggests nitrogen dioxide is an active species.
- Nishiguchi, Takeshi,Bougauchi, Masahiro
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p. 5606 - 5609
(2007/10/02)
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