- Single step transformation of PMB ethers to bromides using a CBr4-TPP reagent system
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PMB ethers are efficiently transformed to their corresponding bromides by a CBr4-TPP reagent system with a wide range of other functional groups also present in the substrate.
- Yadav,Mishra, Rajesh Kumar
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Read Online
- Development of a non-hydroxamate dual matrix metalloproteinase (MMP)-7/-13 inhibitor
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Matrix metalloproteinase 7 (MMP-7) is a member of the MMP superfamily and is able to degrade extracellular matrix proteins such as casein, gelatin, fibronectin and proteoglycan. MMP-7 is a validated target for the development of small molecule drugs against cancer. MMP-13 is within the enzyme class the most efficient contributor to type II collagen degeneration and is a validated target in arthritis and cancer. We have developed the dual MMP-7/-13 inhibitor ZHAWOC6941 with IC50-values of 2.2 μM (MMP-7) and 1.2 μM (MMP-13) that is selective over a broad range of MMP isoforms. It spares MMP-1, -2, -3, -8, -9, -12 and -14, making it a valuable modulator for targeted polypharmacology approaches.
- Fischer, Thomas,Riedl, Rainer
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- COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF AGENTS
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The disclosure features amino lipids and compositions involving the same. Nanoparticle compositions include an amino lipid as well as additional lipids such as phospholipids, structural lipids, PEG lipids, or a combination thereof. Nanoparticle compositions further including therapeutic and/or prophylactic agents such as RNA are useful in the delivery of therapeutic and/or prophylactic agents to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
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Page/Page column 0012
(2017/07/14)
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- Highly efficient preparation of selectively isotope cluster-labeled long chain fatty acids via two consecutive Csp3-Csp3 cross-coupling reactions
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An efficient synthesis involving two copper-catalyzed alkyl-alkyl coupling reactions has been designed to easily access doubly isotope-labeled fatty acids. Such NMR- and IR-active compounds were obtained in excellent overall yields and will be further used for determining the conformation of an alkyl chain of lipidic biomolecules upon interaction with proteins.
- Lethu, Sebastien,Matsuoka, Shigeru,Murata, Michio
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supporting information
p. 844 - 847
(2014/03/21)
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- MULTIFUNCTIONAL RADICAL QUENCHERS AND THEIR USE
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The present disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.
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Page/Page column 35-36
(2011/09/19)
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- Effects of indole fatty alcohols on the differentiation of neural stem cell derived neurospheres
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In a search for inducers of neuronal differentiation to treat neurodegenerative diseases such as Alzheimer's disease, a series of indole fatty alcohols (IFAs) were prepared, 13c (n = 18) was able to promote the differentiation of neural stem cell derived neurospheres into neurons at a concentration of 10 nM. Analysis of the expression of the Notch pathway genes in neurospheres treated during the differentiation phase with 13c (n = 18) revealed a significant decrease in the transcription of the Notch 4 receptor.
- Coowar, Djalil,Bouissac, Julien,Hanbali, Mazen,Paschaki, Marie,Mohier, Eliane,Luu, Bang
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p. 6270 - 6282
(2007/10/03)
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- Chiral discrimination of branched-chain fatty acids by reversed-phase HPLC after labeling with a chiral fluorescent conversion reagent
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Anteiso fatty acids having 16 to 29 carbon atoms were labeled with the chiral fluorescent conversion reagents, (1R,2R)- and (1S,2S)-2-(2,3- anthracenedicarboximido)-cyclohexanol. The diastereomeric esters of anteiso acids having up to 20 carbon atoms were
- Akasaka, Kazuaki,Ohrui, Hiroshi
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p. 153 - 158
(2007/10/03)
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- Monolayers as models for supported catalysts: Zirconium phosphonate films containing manganese(III) porphyrins
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Organized monolayer films of a manganese tetraphenylporphyrin have been prepared and used as supported oxidation catalysts. Manganese 5,10,15,20- tetrakis(tetrafluorophenyl-4′-octadecyloxyphosphonic acid) porphyrin (1) has been immobilized as a monolayer film by a combination of Langmuir-Blodgett (LB) and self-assembled monolayer techniques that use zirconium phosphonate linkages to bind the molecule to the surface. Analysis by FTIR, XPS, UV - vis and polarized optical spectroscopy show that the films consist of noninteracting molecules effectively anchored and oriented nearly parallel to the surface. The monolayer films are stable to the solvent and temperature conditions needed to explore organic oxidations. The activity of films of 1 toward the epoxidation of cyclooctene using iodosylbenzene as the oxidant was compared to that of Manganese 5,10,15,20- tetrakis(pentafluorophenyl) porphyrin (2) and 1 under equivalent homogeneous conditions. The immobilized porphyrin 1 shows an enhanced activity relative to either homogeneous reaction. The main difference between 1 and 2 is the four alkyl phosphonate arms in 1 designed to incorporate the porphyrin within the films. The increased activity of immobilized 1 is a combination of the porphyrin structure, which prohibits the formation of μ-oxo dimers even in solution, and a change in conformation when anchored to the surface. The study demonstrates that careful monolayer studies can provide useful models for the design and study of supported molecular catalyst systems.
- Benitez, Isa O.,Bujoli, Bruno,Camus, Laurent J.,Lee, Christine M.,Odobel, Fabrice,Talham, Daniel R.
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p. 4363 - 4370
(2007/10/03)
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- Double-Headed Haptens with Pyrocatechol (Poison Ivy like) and Methylene Lactone Functional Groups: A Search for Skin-Tolerance Inducers
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In order to develop new theories for desensitization, a potential skin sensitizer, 1, with two different haptenic ends, (a) a pyrocatechol group and (b) an α-methylene-γ-butyrolactone moiety, separated by a straight nine-carbon-atom chain has been prepare
- Mattes, Henri,Benezra, Claude
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p. 165 - 168
(2007/10/02)
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