1242184-48-0Relevant articles and documents
Synthesis of novel N-heterocyclic compounds containing 1,2,3-triazole ring system via domino, “click” and RDA reactions
Palkó, Márta,Haimer, Mohamed El,Kormányos, Zsanett,Fül?p, Ferenc
, (2019/02/26)
An uncomplicated, high-yielding synthetic route has been developed to constitute complicated heterocycles, applying domino, click and retro-Diels–Alder (RDA) reaction sequences. Starting from 2-aminocarboxamides, a new set of isoindolo[2,1-a]quinazolinones was synthesized with domino ring closure. A click reaction was performed to create the 1,2,3-triazole heterocyclic ring, followed by an RDA reaction resulting in dihydropyrimido[2,1-a]isoindole-2,6-diones. The absolute configuration, concluded by the norbornene structure that served as a chiral source, remained constant throughout the transformations. The structure of the synthesized compounds was examined by1H and13C Nuclear Magnetic Resonance (NMR) methods.
Mediators of hedgehog signaling pathways, compositions and uses related thereto
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Page/Page column 77; 78, (2015/11/27)
The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function by contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize hedgehog activity.
Development and scale-up of an optimized route to the ALK inhibitor CEP-28122
Allwein, Shawn P.,Roemmele, Renee C.,Haley, James J.,Mowrey, Dale R.,Petrillo, Daniel E.,Reif, James J.,Gingrich, Diane E.,Bakale, Roger P.
, p. 148 - 155 (2012/05/20)
Evolution of the process strategies to prepare CEP-28122, an anaplastic lymphoma kinase (ALK) inhibitor, is presented. The initial medicinal chemistry route, used for the preparation of key supplies for biological screening, is reviewed. In addition, the
Backbone regulation mimicry by β-peptidic foldamers: formation of a 10-helix in a mixed 6-strand/14-helix conformational pool
Jagadeesh, Bharatam,Kiran, Marelli Udaya,Sudhakar, Ambadi,Chandrasekhar, Srivari
scheme or table, p. 12592 - 12595 (2010/06/21)
A highly robust 6-strand transforms into a right-handed 10-helix through the substitution of 14-helical nucleating residues at alternate positions along the backbone of the oligomer has been reported. The heterooligomers, tetramer and hexamer with NAA and
Potent inhibitors of the Hedgehog signaling pathway
Brunton, Shirley A.,Stibbard, John H. A.,Rubin, Lee L.,Kruse, Lawrence I.,Guicherit, Oivin M.,Boyd, Edward A.,Price, Steven
, p. 1108 - 1110 (2008/09/19)
A small family of phenyl quinazolinone ureas is reported as potent modulators of Hedgehog protein function. Preliminary SAR studies of the urea substituent led to a nanomolar Hedgehog antagonist.
Oligomers of cis-β-norbornene amino acid: Formation of β-strand mimetics
Chandrasekhar, Srivari,Babu, Bathini Nagendra,Prabhakar, Anabathula,Sudhakar, Ambadi,Reddy, Marepally Srinivasa,Kiran, Marelli Udaya,Jagadeesh, Bharatam
, p. 1548 - 1550 (2008/03/12)
The oligomers of constrained cis-exo-β-norbornene amino acid were synthesised and characterised by extensive NMR, CD, IR and MD studies. The results showed the formation of both right and left handed consecutive 6-membered hydrogen-bonded strands for [2S,
Synthesis and stereostructure of 3-amino-5- and -6-hydroxybicyclo[2.2.1] heptane-2-carboxylic acid diastereomers
Palko, Marta,Sandor, Elvira,Sohar, Pal,Fueloep, Ferenc
, p. 2051 - 2058 (2007/10/03)
All-endo-3-amino-5-hydroxybicyclo[2.2.1]heptane-2-carboxylic acid and two epimers of 3-amino-6-hydroxybicyclo[2.2.1]heptane-2-carboxylic acid were prepared via 1,3-oxazine or γ-lactone intermediates by the stereoselective functionalization of endo-3-aminobicyclo[2.2.1]hept-5-ene-2-carboxylic acid derivatives. Their structures were proved by IR and NMR spectroscopy, with the use of HMQC, HMBC, DEPT, and DIFFNOE techniques. Springer-Verlag 2005.
Caspase inhibitors and uses thereof
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Page 17; 18, (2008/06/13)
This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula I: where R1, R2, and R3 are as described herein, Ring A contains zero to two double bonds, each X is independently selected from nitrogen or carbon, at least one X in Ring A is a nitrogen, Ring A is optionally substituted as described, and may be fused to a saturated or unsaturated five to seven membered ring containing zero to three heteroatoms, and provided that when X3 is a carbon, a substituent on X3 is attached by an atom other than nitrogen.
Mediators of hedgehog signaling pathways, compositions and uses related thereto
-
, (2008/06/13)
The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function by contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growt
A convenient synthesis of bridged azatricyclic anhydrides
Canonne,Akssira,Dahdouh,Kasmi,Boumzebra
, p. 1985 - 1992 (2007/10/02)
Bridged N-protected β-amino acids have been regioselectively prepared from the corresponding bicyclic monoesters. The subsequent cyclisation by thionyl chloride produced the desired bridged azatricyclic anhydrides which are versatile substrates for the synthesis of dipeptides; they are also converted into oxathymine and oxauracil by a thermal [4+2] cycloreversion.
