1219937-82-2Relevant academic research and scientific papers
Discovery of a novel series of potent S1P1 agonists
Crosignani, Stefano,Bombrun, Agnes,Covini, David,Maio, Maurizio,Marin, Delphine,Quattropani, Anna,Swinnen, Dominique,Simpson, Don,Sauer, Wolfgang,Fran?on, Bernard,Martin, Thierry,Cambet, Yves,Nichols, Anthony,Martinou, Isabelle,Burgat-Charvillon, Fabienne,Rivron, Delphine,Donini, Cristina,Schott, Olivier,Eligert, Valerie,Novo-Perez, Laurence,Vitte, Pierre-Alain,Arrighi, Jean-Fran?ois
supporting information; experimental part, p. 1516 - 1519 (2010/06/21)
The discovery of a novel series of S1P1 agonists is described. Starting from a micromolar HTS positive, iterative optimization gave rise to several single-digit nanomolar S1P1 agonists. The compounds were able to induce internalization of the S1P1 receptor, and a selected compound was shown to be able to induce lymphopenia in mice after oral dosing.
