Epoxysuccinyl peptide-derived cathepsin B inhibitors: Modulating membrane permeability by conjugation with the C-terminal heptapeptide segment of penetratin [PDF]
Besides its physiological role in lysosomal protein breakdown, extralysosomal cathepsin B has recently been implicated in apoptotic cell death. Highly specific irreversible cathepsin B inhibitors that are readily cellpermeant should be useful tools to ...
Assfalg-Machleidt, Irmgard+5 more
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A Native Hymenopteran Predator of \u3ci\u3eAgonopterix Alstroemeriana\u3c/i\u3e (Lepidoptera: Oecophoridae) in East-Central Illinois [PDF]
Agonopterix alstroemeriana is a European oecophorid moth that defoliates poison hemlock (Conium maculatum), a noxious Eurasian weed extensively naturalized throughout temperate Australia, New Zealand, North America, and South America.
Berenbaum, May R+2 more
core +2 more sources
Orally Active MMP-1 Sparing α-tetrahydropyranyl and α-piperidinyl Sulfone Matrix Metalloproteinase (MMP) Inhibitors with Efficacy in Cancer, Arthritis, and Cardiovascular Disease [PDF]
α-Sulfone-α-piperidine and α-tetrahydropyranyl hydroxamates were explored that are potent inhibitors of MMP’s-2, -9, and -13 that spare MMP-1, with oral efficacy in inhibiting tumor growth in mice and left-ventricular hypertrophy in rats and in the ...
Barta, Thomas E.+3 more
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Nanomolar-potency 'co-potentiator' therapy for cystic fibrosis caused by a defined subset of minimal function CFTR mutants. [PDF]
Available CFTR modulators provide no therapeutic benefit for cystic fibrosis (CF) caused by many loss-of-function mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel, including N1303K. We previously introduced the
Finkbeiner, Walter E+7 more
core
Pot, atom and step economic (PASE) synthesis of highly functionalized piperidines: a five-component condensation [PDF]
The diastereoselective pot, atom and step economic (PASE) synthesis of highly functionalized piperidines has been realized. The procedure simply involves mixing methyl acetoacetate, 2 equiv of aldehyde and 2 equiv of aniline together in the presence of ...
Clarke, Paul A.+2 more
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Synthesis and characterization of the N-terminal acetylated 17-23 fragment of thymosin beta 4 identified in TB-500, a product suspected to possess doping potential [PDF]
A
Esposito+12 more
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Synthesis of dihydropyridine and piperidine derivatives via an unexpected reaction of pyridine with acetyl chloride [PDF]
Acetyl chloride reacts with pyridine to give a mixture of N-acetyl-1,4- and 1,2-dihydropyridyl acetic acid (1a,b) after water quenching. The reactioninvolves the formation of a zwitterionic ketene enolate intermediate which results from deprotonation of
Mannu, Alberto+2 more
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\u3ci\u3eAgonopterix Alstroemeriana\u3c/i\u3e (Oecophoridae) and Other Lepidopteran Associates of Poison Hemlock \u3ci\u3e(Conium Maculatum)\u3c/i\u3e in East Central Illinois [PDF]
Poison hemlock (Conium maculatum) (Apiaceae), a noxious Eurasian weed extensively naturalized throughout North America, is characteristically attacked by few insects.
Berenbaum, May R, Harrison, Terry L
core +2 more sources
Reactive organoallyl species generated from aryl halides and allene: allylation of alpha,beta-unsaturated aldehydes and cyclic ketones employing Pd/In transmetallation processes [PDF]
Allylation of α,β-unsaturated aldehydes and cyclic ketones promoted by Pd/In transmetallation processes has been studied. The unsaturated aldehydes underwent regioselective 1,2-addition to afford secondary homoally alcohols.
Anwar+56 more
core +2 more sources