149967-07-7Relevant articles and documents
Asymmetric Synthesis of a New Proline Analogue
Vasella, Andrea,Voeffray, Robert
, p. 97 - 98 (1981)
The 1,3-dipolar cycloaddition to ethylene of N-glycosylnitrones, formed in situ from the partially protected D-mannose- or D-ribose-oximes and various glyoxalates, gave compounds which could be transformed into both enantiomers of 3-t-butoxycarbonyl-isoxazolidine and derivatives thereof.
NOVEL HISTONE METHYLTRANSFERASE INHIBITORS
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Page/Page column 30; 68, (2021/04/01)
The present invention relates to novel compounds of formula (I) as defined herein. The compounds are inhibitors of histone methyltransferases of the seven-beta-strand family, in particular of KMT9.
PI3K INHIBITORS AND USES THEREOF
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Paragraph 00450-00451, (2020/05/15)
The development of a new, targeted drug delivery paradigm coupled to improved PI3K inhibitors (e.g., PI3Kα inhibitors) represents a significant advance in cancer therapy. Provided herein are compounds, such as compounds of Formula (I) and (II), and pharmaceutically acceptable salts, hydrates, solvates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The compounds provided herein are PI3K (e.g., PI3Kα) inhibitors and are therefore useful for the treatment and/or prevention of various diseases (e.g., proliferative diseases such as cancer). Also provided herein are nanoparticles and nanogels (e.g., P-selectin targeting nanoparticles) comprising PI3K inhibitors, such a compound described herein. In certain embodiments, a nanoparticle or nanogel described herein encapsulates a compound described herein for targeting delivery to cancer cells or tumors.
Synthesis of desmosine-containing cyclic peptide for the possible elucidation of elastin crosslinking structure
Ogawa, Keita,Hayashi, Takahiro,Lin, Yong Y.,Usuki, Toyonobu
, p. 3838 - 3847 (2017/06/13)
Elastin is a vital extracellular matrix protein, which is known for providing elasticity in numerous tissues. It is formed by the self-assembly and subsequent crosslinking of elastin precursor, tropoelastin. Two tetrafunctional, pyridinium-based amino acids desmosine and isodesmosine are exclusively found in elastin and play an important role as crosslinkers. Structural elucidation of elastin has eluded scientists to date, owing to the highly cross-linked structure and insoluble nature. Therefore, in this study, we aimed to synthesize a desmosine-containing cyclic peptide as a partial elastin mimic, in order to eventually facilitate the elucidation of the crosslinking pattern of elastin by mass spectrometric analysis.
PSMA INHIBITORS
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Paragraph 0176, (2013/12/03)
Compounds as defined herein are provided which are useful in (1) diagnostic methods for detecting and/or identifying cells presenting PSMA; and (2) methods for preparing the compounds.
Nicotianamine-Derived Metallophore And Processes For Producing Same
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Page/Page column 2, (2012/04/23)
The invention relates to a nicotianamine derivative and to a process for chemical or enzymatic synthesis thereof. The nicotianamine derivative has the following formula (I). The invention finds use in the pharmacy field in particular.
The crystallographic structure of thermoNicotianamine synthase with a synthetic reaction intermediate highlights the sequential processing mechanism
Dreyfus, Cyril,Larrouy, Manuel,Cavelier, Florine,Martinez, Jean,Pignol, David,Arnoux, Pascal
supporting information; experimental part, p. 5825 - 5827 (2011/06/23)
We determined the three-dimensional structure of a complex between an archaeal nicotianamine synthase homologue and a chemically synthesised reaction intermediate. This structure suggests that the enzymes cavity allows both an ordered substrate binding an
Efficient synthesis of nicotianamine and non-natural analogues
Bouazaoui, M'Barek,Larrouy, Manuel,Martinez, Jean,Cavelier, Florine
experimental part, p. 6609 - 6617 (2011/02/25)
An efficient synthesis of nicotianamine has been achieved by using a new strategy based on N-alkylation. Sulfonamide activation proved to be necessary for the alkylation of the primary amine and the 2-(trimethylsilyl)ethanesulfonyl group was easily introd
Synthesis of an Fmoc-Asn-heptasaccharide building block and its application to chemoenzymatic glycopeptide synthesis
Mezzato, Stefano,Unverzagt, Carlo
experimental part, p. 1306 - 1315 (2010/10/02)
The Fmoc-protected heptasaccharide asparagine building block β-GlcNAc-(1→2)-α-Man-(1→3)-[β-GlcNAc-(1→2) -α-Man-(1→6)]β-Man-(1→4)-β-GlcNAc-(1→4) -β-GlcNAc-(Fmoc)Asn was obtained by chemical synthesis. Two flexible strategies were developed with optimized c
Direct access to L-azetidine-2-carboxylic acid
Bouazaoui, M'barek,Martinez, Jean,Cavelier, Florine
experimental part, p. 2729 - 2732 (2009/08/16)
A straightforward synthesis of L-azetidine-2-carboxylic acid is described, leading to both orthogonally protected versions or totally deprotected L-Aze. The starting material is a commercially available aspartic acid derivative, whose chirality is conserv