- HDAC INHIBITOR COMPOUNDS AND METHODS OF TREATMENT
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The instant invention describes hydrazide-containing compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders, or affect cell differentiation, dedifferentiation or transdiffer
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Page/Page column 36; 37; 40
(2015/11/17)
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- Alkylation of Amines with Alcohols and Amines by a Single Catalyst under Mild Conditions
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An efficient catalytic system for the alkylation of amines with either alcohols or amines under mild conditions has been developed, using cyclometallated iridium complexes as catalysts. The method has broad substrate scope, allowing for the synthesis of a diverse range of secondary and tertiary amines with good to excellent yields. By controlling the ratio of substrates, both mono- and bis-alkylated amines can be obtained with high selectivity. In particular, methanol can be used as the alkylating reagent, affording N-methylated products selectively. A strong solvent effect is observed for the reaction.
- Zou, Qingzhu,Wang, Chao,Smith, Jen,Xue, Dong,Xiao, Jianliang
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supporting information
p. 9656 - 9661
(2015/06/30)
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- Discovery of a novel series of indolyl hydrazide derivatives as diacylglycerol acyltransferase-1 inhibitors
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A novel series of hydrazide derivatives were synthesized as potential diacylglycerol acyltransferase (DGAT) inhibitors. Among them, compounds 8u and 8v exhibited selective and potent DGAT-1 inhibitory activities. In addition, compound 8u dose-dependently inhibited triglyceride synthesis in HepG2 cell lines. Furthermore, treatment with compound 8u for an oral lipid tolerance test showed a significant decrease in plasma triglyceride levels compared with vehicle-treated control animals, indicating delayed absorption of triglyceride after an acute lipid challenge.
- Kim, Minkyoung,Kwon, Jinsun,Kim, Mun Ock,Singh, Sarbjit,Kim, Sang Kyum,Lee, Kyeong,Lee, Kiho,Lee, Hyun Sun,Choi, Yongseok
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p. 628 - 635
(2015/05/04)
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- The α-effect in iminium ion catalysis
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The α-effect can be used as an effective means to promote iminium ion catalysed transformations, providing acyclic scaffolds to aid in catalyst design. A thorough investigation of the structure-activity relationship of the catalyst architecture reveals optimal substituents of a disubstituted carbamate and a secondary alkyl group around a hydrazine scaffold. Molecular modelling investigations provide a mechanistic rationale to the results observed.
- Cavill, Julie L.,Elliott, Richard L.,Evans, Gareth,Jones, Ian L.,Platts, James A.,Ruda, Antonio M.,Tomkinson, Nicholas C. O.
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p. 410 - 421
(2007/10/03)
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- An efficient synthesis of substituted hydrazides
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Routes for the selective synthesis of 1-, or 2-substituted hydrazides, and 1,2-disubstituted hydrazides are reported. These routes proceed via cyanoborohydride reduction of stable acyl hydrazone intermediates. Georg Thieme Verlag Stuttgart.
- Benstead, David J.,Hulme, Alison N.,McNab, Hamish,Wight, Paul
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p. 1571 - 1574
(2007/10/03)
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- Iminium ion catalysis: Use of the α-effect in the acceleration of the Diels-Alder reaction
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The α-effect can be used in the acceleration of the DielsAlder reaction between a series of dienes and electron deficient dienophiles using iminium ion catalysis, providing a novel molecular scaffold capable of performing this class of catalytic process.
- Cavill, Julie L.,Peters, Jens-Uwe,Tomkinson, Nicholas C. O.
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p. 728 - 729
(2007/10/03)
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