847663-65-4Relevant academic research and scientific papers
Amide-to-ester substitution allows fine-tuning of the cyclopeptide conformational ensemble
Cupido, Tommaso,Spengler, Jan,Ruiz-Rodriguez, Javier,Adan, Jaume,Mitjans, Francesc,Piulats, Jaume,Albericio, Fernando
, p. 2732 - 2737 (2010)
(Figure Presented) Without affecting the overall 3D structure, amide-to-ester backbone substitution (or ester scan) exerts a pronounced influence on the conformational equilibrium of the RCD cyclopeptide cilengitide and its derivatives (see figure; RGD = Arg-GlyAsp). The appropriate substitution, which stabilized the receptor-complementary conformations, improved the biological activity of this integrin antagonist.
A new strategy for solid-phase depsipeptide synthesis using recoverable building blocks
Albericio, Fernando,Burger, Klaus,Ruiz-Rodriguez, Javier,Spengler, Jan
, p. 597 - 600 (2007/10/03)
(Chemical Equation Presented) The technique of choice for synthesis of small-scale depsipeptides is on a solid support. However, if expensive monomers have to be incorporated, solid-phase synthesis can quickly turn out to be unattractive because of its lo
