892128-58-4Relevant articles and documents
A inhibiting DPP-IV compounds and intermediates
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, (2016/10/20)
Provided are compounds as presented in formulas IA or IB or pharmaceutically acceptable salts thereof, the preparation method therefor, and uses thereof. Also provided are the intermediates of the compounds and the preparation method therefor. The compounds of the present invention can effectively inhibit DPP-IV activity. Compared to the commercial available medicine, Januvia, compound 1 exhibits strong inhibition against DPP4, but has lower activity inhibition against other DPP family members (DPP2, DPP8, and DPP9). Hence the compound of the present invention can not only effectively inhibit DPP4 from exhibiting medicinal activity, but also lower the activity inhibition against other members of the DPP family, reduce toxic side effect, and have better medicinal safety.
Collagen labelling with an azide-proline chemical reporter in live cells
Amgarten, Beatrice,Rajan, Rakesh,Martínez-Sáez, Nuria,Oliveira, Bruno L.,Albuquerque, Inês S.,Brooks, Roger A.,Reid, David G.,Duer, Melinda J.,Bernardes, Gon?alo J. L.
supporting information, p. 5250 - 5252 (2015/03/30)
We have developed a strategy for selective imaging of collagen in live foetal ovine osteoblasts. Our approach involves the incorporation of an azide-tagged proline in the biosynthesis of collagen followed by labelling using a strain-promoted [3+2] azide-alkyne cycloaddition reaction. This journal is
Functionalizable oligoprolines as molecular scaffolds
Nagel, Yvonne A.,Kuemin, Michael,Wennemers, Helma
, p. 264 - 267 (2011/12/21)
Azidoproline (Azp) containing oligoprolines are conformationally well-defined, helical molecular scaffolds that allow for facile functionalization. Within this article we describe the synthesis of Azp-containing oligoprolines and different strategies to introduce functional moieties. In addition, the influence of factors such as substituents at the γ-position of proline as well as functional groups at the termini on the conformational stability of the molecular scaffolds are briefly presented. Schweizerische Chemische Gesellschaft.
Solid-phase synthesis of an apoptosis-inducing tetrapeptide mimicking the Smac protein
Le Quement, Sebastian T.,Ishoey, Mette,Petersen, Mette T.,Simonsen, Pernille M.,Holck, Nanna S.,Nielsen, Thomas E.
, p. 7049 - 7053 (2012/01/13)
An approach for the solid-phase synthesis of apoptosis-inducing Smac peptidomimetics is presented. Using a Rink linker strategy, tetrapeptides mimicking the N-4-terminal residue of the Smac protein [(N-Me)AVPF sequence] were synthesized on PEGA resin in excellent purities and yields. Following two synthetic routes, a known tetrapeptide, incorporating a substituted proline, previously shown to exhibit excellent biological activity in vitro as well as low toxicity, was synthesized effectively on a solid support.
Solid-phase synthesis of smac peptidomimetics incorporating triazoloprolines and biarylalanines
Le Quement, Sebastian T.,Ishoey, Mette,Petersen, Mette T.,Thastrup, Jacob,Hagel, Grith,Nielsen, Thomas E.
, p. 667 - 675 (2012/03/22)
Apoptotic induction mechanisms are of crucial importance for the general homeostasis of multicellular organisms. In cancer the apoptotic pathways are downregulated, which, at least partly, is due to an abundance of inhibitors of apoptosis proteins (IAPs) that block the apoptotic cascade by deactivating proteolytic caspases. The Smac protein has an antagonistic effect on IAPs, thus providing structural clues for the synthesis of new pro-apoptotic compounds. Herein, we report a solid-phase approach for the synthesis of Smac-derived tetrapeptide libraries. On the basis of a common (N-Me)AVPF sequence, peptides incorporating triazoloprolines and biarylalanines were synthesized by means of Cu(I)-catalyzed azide-alkyne cycloaddition and Pd-catalyzed Suzuki cross-coupling reactions. Solid-phase procedures were optimized to high efficiency, thus accessing all products in excellent crude purities and yields (both typically above 90%). The peptides were subjected to biological evaluation in a live/dead cellular assay which revealed that structural decorations on the AVPF sequence indeed are highly important for cytotoxicity toward HeLa cells.
PYRROLOTRIAZINE KINASE INHIBITORS
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Page/Page column 97, (2011/04/19)
The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
Total synthesis and antifungal evaluation of cyclic aminohexapeptides
Klein, Larry L.,Li, Leping,Chen, Hui-Ju,Curty, Cynthia B.,Degoey, David A.,Grampovnik, David J.,Leone, Christina L.,Thomas, Sheela A.,Yeung, Clinton M.,Funk, Kenneth W.,Kishore, Vimal,Lundell, Edwin O.,Wodka, Dariusz,Meulbroek, Jon A.,Alder, Jeffrey D.,Nilius, Angela M.,Lartey, Paul A.,Plattner, Jacob J.
, p. 1677 - 1696 (2007/10/03)
The need for new therapies to treat systemic fungal infections continues to rise. Naturally occurring hexapeptide echinocandin B (1) has shown potent antifungal activity via its inhibition of the synthesis of β-1,3 glucan, a key fungal cell wall component. Although this series of agents has been limited thus far based on their physicochemical characteristics, we have found that the synthesis of analogues bearing an aminoproline residue in the 'northwest' position imparts greatly improved water solubility (>5 mg/mL). The synthesis and structure-activity relationships (SAR) based on whole cell and upon in vivo activity of the series of compounds are reported. Copyright (C) 2000 Elsevier Science Ltd.
