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The highly efficient and diastereoselective synthesis of E dienes has been accomplished through radical cyclization of bromoallyl hydrazones. This methodology has been further extended to generate these products through a one-pot condensation/radical cyclization/cycloreversion cascade from simple aldehyde starting materials in high yields (>75 %) and high diastereoselectivities (>95:5). Mechanistic investigations suggest that the cascade reaction proceeds through a cyclic diazene intermediate prior to the cycloreversion.

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Reference:
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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The key is symmetry! A convergent synthetic approach of the highly cytotoxic natural product (-)-callystatin A was developed assembling three fragments through Julia-Kocienski olefination and Stille cross-coupling. The new strategy relies on a pivotal local symmetry of the target molecule. In this preliminary study, particular attention was devoted to facilitate the catalytic enantiocontrol of strategic stereogenic centers present in each of the fragments (see scheme). Copyright

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Reference:
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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This invention relates to Group 4 catalyst compounds containing di-anionic tridentate nitrogen/oxygen based ligands. The catalyst compounds are useful, with or without activators, to polymerize olefins, particularly a-olefins, or other unsaturated monomers. Systems and processes to oligomerize and/or polymerize one or more unsaturated monomers using the catalyst compound, as well as the oligomers and/or polymers produced therefrom are also provided.

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Reference:
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Bisphosphonate squalene synthetase inhibitors and method

Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents are provided which have the structure STR1 and analogs thereof, wherein R1, R2, R3 and R4 are the same or different and are H, lower alkyl, a metal ion or a prodrug ester; R5 is H, halogen or lower alkyl; Zq is substituted alkenyl, substituted alkynyl, mixed alkenyl-alkynyl or substituted phenylalkyl or, phenylalkenyl or phenylalkynyl, or alkyl, including all stereoisomers thereof. New methods for using such compounds to inhibit cholesterol biosynthesis are also provided.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Differential effect of wortmannolone derivatives on MDA-MB-231 breast cancer cells

Background/Aim: The survival rate of women diagnosed with triple-negative breast-cancer (TNBC) remains low. Hence, this study aimed at the chemical and biological optimization of furanosteroid derivatives for the treatment of this type of malignancy using TNBC cells. Materials and Methods: Semi-synthetic analogs of wortmannolone (1-6) that negatively affected the aberrant pathways in tumor cells were evaluated in hormoneindependent breast cancer cells using western blot and cellcycle analysis. Results: Wortmannolone derivatization generated NF-?B inhibitors as new lead structures for further development. Compound (3) was found to be the most significantly active lead. Conclusion: Structure-activity analysis in the present study showed that acetylation of the hydroxyl groups and substitution on C3 and C17 of wortmannolone enhanced biological activity. Alphasubstitution of the acetyl group in C3 on ring A (compound 3) resulted in ROS inducing effect; however, presence of an acetyl group in beta-position of C3 displayed the highest NF-?B p65 inhibitory activity (0.60 muM).

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Aminocyclohexane derivatives as 5-HT receptor agonists

A class of substituted aminocyclohexane derivatives are selective agonists of 5-HT 1 -like receptors, being potent agonists of the human 5-HT 1D alpha receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT 1D alpha receptor subtype relative to the 5-HT 1D beta subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT 1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT 1D receptor agonists.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Highly efficient use of NaOCI in the Ru-catalysed oxidation of aliphatic ethers to esters

The selectivity of alpha-oxidation of ethers to esters via RuNaOCI can be dramatically improved by pH control, at high substrate to catalyst ratios using a stoichiometric amount of hypochlorite in biphasic media at room temperature.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Methods and compositions for treating preterm labor

The present invention provides for a method of treating preterm labor in a subject in need of such treatment comprising administration of a therapeutically effective amount of an inhibitor of 5alpha-reductase type 1 to the subject. The present invention further provides for a method of preventing premature labor in a subject susceptible thereto comprising administration of a labor-preventive amount of an inhibitor of 5alpha-reductase type 1 to the subject. Further, the present invention also relates to a method of reducing the risk of premature labor in a subject at risk therefor. The present invention also provides for a method for stopping labor preparatory (i.e., prior) to Cesarean delivery in a subject in need of such treatment comprising administration of a therapeutically effective amount of an inhibitor of 5alpha-reductase type 1 to the subject. Further, the present invention provides for compositions useful in the methods of the present invention, as well as a method of manufacture of a medicament useful for treating pre-term labor and for stopping labor preparatory to Cesarean delivery.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Recent developments in catalytic alcohol oxidation using nitroxyl radicals

This chapter describes the use of nitroxyl radicals as catalysts for the oxidation of alcohols, with a focus on recent developments in this area. Stable nitroxyl radicals can be used with a variety of different terminal oxidants and the methods discussed have a much greater substrate scope compared to precious-metal catalysts. The methods are readily accessible for small-scale applications as they use commercially available reagents and do not require high pressures or temperatures. This review not only describes the selective oxidation of alcohols to aldehydes, ketones, and carboxylic acids, but also reactions where alcohol oxidation is a key step, such as the oxidative synthesis of nitriles, imines, and amides.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Stereo- and regio-selective synthesis of 3?-: C -substituted-(N)-methanocarba adenosines as potential anticancer agents

Stereo- and regio-selective synthesis of 3?-C-substituted-(N)-methanocarba adenosines 3a-c as potential anticancer agents was achieved by employing stereoselective cyclopropanation, stereoselective nucleophilic addition, regioselective isopropylidene cleavage and regioselective base condensation of cyclic sulfate as key steps.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI