- Novel Substituted Poly(benzothiophenes); Controlling the n- and p-Doping Potentials
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Methyl-, chloro- and fluoro-substitution in the C6 ring has little effect on the oxidation of polybenzothiophene films to the p-doped conducting form, but has a marked effect on reduction to the n-doped form; poly(5,6-dichlorobenzothiophene) is n-do
- King, Geoff,Higgins, Simon J.
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Read Online
- CYCLIC PEPTIDE ANALOGS OF MELANOCORTIN AND AMANITIN AND METHODS OF MAKING SUCH
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The invention described herein is based in part on the discovery of a protein/peptide crosslink, which introduces fluorescent properties, and which has been applied to synthesize analogues of melanocortin and amanitin as choice peptides to be explored in the context of isoindole peptides. Without limitation, it is expected that those trained in the art of peptide synthesis and stapling would appreciate the consequences of this invention such that other peptides of varied length can be similarly constrained by isoindole staples as featured herein.
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Paragraph 0114; 0116-0117; 0120
(2021/01/29)
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- Fluorescent Isoindole Crosslink (FlICk) Chemistry: A Rapid, User-friendly Stapling Reaction
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The stabilization of peptide secondary structure via stapling is a ubiquitous goal for creating new probes, imaging agents, and drugs. Inspired by indole-derived crosslinks found in natural peptide toxins, we employed ortho-phthalaldehydes to create isoindole staples, thus transforming inactive linear and monocyclic precursors into bioactive monocyclic and bicyclic products. Mild, metal-free conditions give an array of macrocyclic α-melanocyte-stimulating hormone (α-MSH) derivatives, of which several isoindole-stapled α-MSH analogues (Ki≈1 nm) are found to be as potent as α-MSH. Analogously, late-stage intra-annular isoindole stapling furnished a bicyclic peptide mimic of α-amanitin that is cytotoxic to CHO cells (IC50=70 μm). Given its user-friendliness, we have termed this approach FlICk (fluorescent isoindole crosslink) chemistry.
- Todorovic, Mihajlo,Schwab, Katerina D.,Zeisler, Jutta,Zhang, Chengcheng,Bénard, Francois,Perrin, David M.
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p. 14120 - 14124
(2019/07/31)
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- Cobalt-Catalyzed Formal [4+2] Cycloaddition of α,α′-Dichloro-ortho-Xylenes with Alkynes
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A formal [4+2] cycloaddition of α,α′-dichloro-ortho-xylenes with various alkynes has been developed using a low-valent cobalt catalyst. The transformation has a wide substrate scope and high functional-group tolerance and led to 1,4-dihydronaphthalenes. T
- Komeyama, Kimihiro,Okamoto, Yuji,Takaki, Ken
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supporting information
p. 11325 - 11328
(2016/02/19)
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- Preparation of dihydropyrrol derivatives as intermediates
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The invention is concerned with a new scalable process for the preparation of compounds of formula I comprising a new process for the preparation of the key intermediate, a dihydropyrrole derivative formula II or a salt thereof.
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Page/Page column 5
(2009/06/27)
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- Isoindolin-1-one glucokinase activators
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Isoindolin-1-one-substituted propionamide glucokinase activators which increase insulin secretion in the treatment of type II diabetes.
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