65638-82-6Relevant articles and documents
Environmentally benign peptide synthesis using liquid-assisted ball-milling: Application to the synthesis of Leu-enkephalin
Bonnamour, Julien,Metro, Thomas-Xavier,Martinez, Jean,Lamaty, Frederic
supporting information, p. 1116 - 1120 (2013/06/05)
This paper describes an original methodology for peptide bond synthesis avoiding toxic solvents and reactants. Ball-milling stoichiometric amounts of Boc-protected α-amino acid N-carboxyanhydrides (Boc-AA-NCA) or Boc-protected α-amino acid N-hydroxysuccin
NOVEL SMALL MOLECULE DNAK INHIBITORS
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Page/Page column 47, (2010/04/30)
Methods of inhibiting HSP70 proteins, agents causing the inhibition of HSP70 proteins, and the effects of such inhibition on cell proliferation. Anti-microbial agents comprising small molecules, or pharmaceutical salts thereof, disclosed herein and furthe
Linear TMC-95-based proteasome inhibitors
Basse, Nicolas,Piguel, Sandrine,Papapostolou, David,Ferrier-Berthelot, Alexandra,Richy, Nicolas,Pagano, Maurice,Sarthou, Pierre,Sobczak-Thépot, Jo?lle,Reboud-Ravaux, Michele,Vidal, Jo?lle
, p. 2842 - 2850 (2008/02/07)
We have designed and evaluated 45 linear analogues of the natural constrained cyclopeptide TMC-95A. These synthetically less demanding molecules are based on the tripeptide sequence Y-N-W of TMC-95A. Structural variations in the amino acid side chains and
Synthesis of Macrocyclic Peptide Analogues of Proteasome Inhibitor TMC-95A
Berthelot, Alexandra,Piguel, Sandrine,Le Dour, Gwennael,Vidal, Joelle
, p. 9835 - 9838 (2007/10/03)
The synthesis of three constrained macrocyclic peptide analogues 1 of TMC-95A as potential proteasome inhibitors is described. The key step involves a Ni(O)-mediated macrocyclization of tripeptides 2 bearing halogenated aromatic side chains for the formation of the biaryl junction. In addition, an enantioselective preparation of L-7-bromotryptophan methyl ester 3 using a Corey-O'Donnell alkylation of the glycine benzophenone imine was achieved in good overall yield with very high ee (>85%) on a multigram scale.