| Literature DB >> 20149651 |
Stefano Crosignani1, Agnes Bombrun, David Covini, Maurizio Maio, Delphine Marin, Anna Quattropani, Dominique Swinnen, Don Simpson, Wolfgang Sauer, Bernard Françon, Thierry Martin, Yves Cambet, Anthony Nichols, Isabelle Martinou, Fabienne Burgat-Charvillon, Delphine Rivron, Cristina Donini, Olivier Schott, Valerie Eligert, Laurence Novo-Perez, Pierre-Alain Vitte, Jean-François Arrighi.
Abstract
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. Copyright 2010 Elsevier Ltd. All rights reserved.Entities:
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Year: 2010 PMID： 20149651 DOI： 10.1016/j.bmcl.2010.01.102
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823