- 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; 82
(2020/07/14)
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- Effect of Substituents and Stability of Transient Aluminum-Aminals in the Presence of Nucleophiles
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Disubstituted hydroxylamines are synthesized and used to form aluminum-amide complexes. These reagents mask carbonyl groups in situ via nucleophilic addition. The stability and utility of the aluminum-aminals are presented in the context of selectively controlling nucleophilic addition on substrates with multiple carbonyl groups.
- Barrios, Francis J.,Springer, Brannon C.,Hazlitt, Robert A.,Colby, David A.
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p. 175 - 180
(2015/05/05)
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- Control of transient aluminum-aminals for masking and unmasking reactive carbonyl groups
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A new reagent, the dimethylaluminum N,O-dimethylhydroxylamine complex, is effective at masking reactive carbonyl groups in situ from nucleophilic addition. This reagent allows chemoselective addition of reducing reagents, Grignard reagents, organolithiums, Wittig reagents, and enolates into substrates with multiple carbonyl groups. Moreover, the trapped carbonyl group, a stable aminal, can be unmasked in situ for additional synthetic manipulations.
- Barrios, Francis J.,Springer, Brannon C.,Colby, David A.
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supporting information
p. 3082 - 3085
(2013/07/26)
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- Dialkylaluminum N, O -dimethylhydroxylamine complex as a reagent to mask reactive carbonyl groups in situ from nucleophiles
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Aluminum complexes of N,O-dimethylhydroxylamine are effective reagents to mask carbonyl groups in situ from nucleophilic addition by organolithiums, Grignard reagents, and borohydrides. The utility of this process by selectively adding nucleophiles into carbonyl groups on a variety of structures as well as distinguishing between carbonyl groups on a sensitive natural product is demonstrated. 1H NMR analysis supports the in situ masking of the more reactive carbonyl group.
- Barrios, Francis J.,Zhang, Xuechao,Colby, David A.
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supporting information; experimental part
p. 5588 - 5591
(2011/02/23)
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- INHIBITORS OF JANUS KINASES
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The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
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Page/Page column 43
(2010/04/03)
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- Phenyl bridging in ring-substituted cumyloxyl radicals. a product and time-resolved kinetic study
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The reactivity of cumyloxyl radicals bearing cyclopropyl and 2,2-diphenylcyclopropyl groups in the para position has been investigated. Depending on radical structure, products deriving from C-C β-scission and/or cyclopropyl ring-opening are observed, sup
- Salamone, Michela,Bietti, Massimo,Calcagni, Alessandra,Gente, Giacomo
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supporting information; experimental part
p. 2453 - 2456
(2009/10/24)
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- Aqueous phase C-H bond oxidation reaction of arylalkanes catalyzed by a water-soluble cationic Ru(III) complex [(pymox-Me2) 2RuCl2]+BF4-
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The cationic complex [(pymox-Me2)RuCl2] -BF4- was found to be a highly effective catalyst for the C-H bond oxidation reaction of arylalkanes in water. For example, the treatment of ethylbenzene (1.0 mmol) with t-BuOOH (3.0 mmol) and 1.0 mol % of the Ru catalyst in water (3 mL) cleanly produced PhCOCH3 at room temperature. Both a large kinetic isotope effect (kH/k D) 14) and a relatively large Hammett value (ρ) -1.1) suggest a solvent-caged oxygen rebounding mechanism via a Ru(IV)-oxo intermediate species.
- Yi, Chae S.,Kwon, Ki-Hyeok,Lee, Do W.
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supporting information; experimental part
p. 1567 - 1569
(2009/08/07)
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- THE IN SITU PROTECTION OF ALDEHYDES VIA α-AMINO ALKOXIDES
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Aromatic and aliphatic aldehydes can be protected in situ via the formation of α-amino alkoxides and their O-trimethylsilyl derivatives.
- Comins, Daniel L.,Brown, Jack D.
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p. 4213 - 4216
(2007/10/02)
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- ELECTRON-TRANSFER PROCESSES BY PEROXYDISULPHATE: HOMOLYTIC BENZYLATION OF QUINONES BY ALKYLARENES AND REACTIONS OF AROMATIC RADICAL CATIONS WITH AROMATICS
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Quinones are monobenzylated in good to satisfactory yields by alkylarenes and the Ag(+)/S2O8(2-) couple under two-phase conditions.Under homogeneous conditions polybenzylation can be obtained.The polar effect of the aromatic substrate substituents in the ring and in the side chain is discussed on the basis of the intermediate aromatic radical cation reactivity in side-chain proton loss and electrophilic aromatic addition.The high efficiency of the quinone system in trapping benzylic radicals, coming from the aromatic radical cations, is ascribed to a charge-transfer transition state.
- Citterio, Attilio
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p. 253 - 258
(2007/10/02)
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