109953-91-5Relevant academic research and scientific papers
NOVEL HIGH AFFINITY QUINOLINE-BASED KINASE LIGANDS
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Paragraph 0237, (2014/01/09)
Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
Microwave-enhanced solid-phase synthesis of N,N′-linked aliphatic oligoureas and related hybrids
Douat-Casassus, Céline,Pulka, Karolina,Claudon, Paul,Guichard, Gilles
supporting information; experimental part, p. 3130 - 3133 (2012/09/08)
A practical and efficient microwave-assisted solid-phase method for the synthesis of N,N′-linked oligoureas and related amide/urea hybrid oligomers, featuring the use of succinimidyl (2-azido-2-substituted ethyl) carbamate monomers, is reported. The rate enhancement of urea formation under microwave irradiation combined with the mild conditions of the phosphine-based azide reduction makes this approach very effective for routine synthesis of oligoureas and possibly for library production.
Synthesis of novel N-protected β3-amino nitriles: study of their hydrolysis involving a nitrilase-catalyzed step
Veitia, Maite Sylla-Iyarreta,Brun, Pierre Louis,Jorda, Pierre,Falguieres, Annie,Ferroud, Clotilde
experimental part, p. 2077 - 2089 (2010/03/04)
Several commercially available nitrilases were investigated with regard to their potential to hydrolyze N-protected β3-amino nitriles into their corresponding N-protected β3-amino acids. The biotransformations were obtained in different proportions depending on the nitrilase involved. The best hydrolysis results were achieved for the N-Cbz-β3-amino nitrile from l-alanine using the NIT-107, in a phosphate buffer at 0.05 M. However, no biotransformation into the corresponding acids was observed for the N-sulfonylamide β3-amino nitriles. Two simple and efficient procedures to prepare the β3-amino nitriles from their analogous α-amino acids are described. Thirty four new substances were synthesized and characterized over the course of this work.
Novel high affinity quinoline-based kinase ligands
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Page/Page column 94; 95, (2008/06/13)
Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
Syntheses of amino alcohols and chiral C2-symmetric bisoxazolines derived from O-alkylated R-4-hydroxyphenylglycine and S-tyrosine
Caplar, Vesna,Raza, Zlata,Katalenic, Darinka,Zinic, Mladen
, p. 23 - 36 (2007/10/03)
Chiral C2-symmetric bisoxazolines 1b-f and 2b,c, derived from 4′-O-alkylated R-4-hydroxyphenylglycine or S-tyrosine, were prepared. As intermediates, a series of chiral amino alcohols possessing substituted phenolic groups was prepared and fully characterized.
Synthesis of a novel β-turn mimetic and its incorporation in Leu- enkephalin
Kreye, Paul,Kihlberg, Jan
, p. 6113 - 6116 (2007/10/03)
A conformationally restricted β-turn mimetic, in which an ethylene bridge replaces the intramolecular hydrogen bond between residues i and i+3 of β-turns, has been prepared and incorporated in Leu-enkephalin. Amino acids and α-bromoacids were used as building blocks in the synthesis of the mimetic.
SYNTHESIS OF ISOSTERIC METHYLENE-OXY PSEUDOPEPTIDE ANALOGUES AS NOVEL AMIDE BOND SURROGATE UNITS
Rubini, E.,Gilon, C.,Selinger, Z.,Chorev, M.
, p. 6039 - 6045 (2007/10/02)
The syntheses of several fully protected dipeptide isosteres which incorporate a methylene-oxy bond replacing the amide bond are described.The novel methylene-oxy modification offers a polar, flexible, proteolytically resistant peptide bond surrogate which can be easily incorporated into biologically active peptides.The standard geometries of the trans-amide, methylene-oxy and methylene-thio units are compared, showing a very close geometrical resemblance of the ψ2-O> unit to the amide bond.
