2. Academic Validation
  3. Biaryl analogues of teriflunomide as potent DHODH inhibitors

Biaryl analogues of teriflunomide as potent DHODH inhibitors

  • Bioorg Med Chem Lett. 2011 Dec 15;21(24):7268-72. doi: 10.1016/j.bmcl.2011.10.052.
Montse Erra 1,  Imma Moreno,  Jordi Sanahuja,  Miriam Andrés,  Raquel F Reinoso,  Estrella Lozoya,  Pilar Pizcueta,  Núria Godessart,  Julio Cesar Castro-Palomino
Affiliations

Affiliation

  • 1 Almirall, R&D Centre, Laureà Miró 408-410, Sant Feliu de Llobregat, 08980 Barcelona, Spain. montse.erra@almirall.com
PMID: 22078215 DOI: 10.1016/j.bmcl.2011.10.052
Abstract

The structure-activity relationships of a novel series of biaryl Dihydroorotate Dehydrogenase (DHODH) inhibitors related to teriflunomide are disclosed. These biaryl derivatives were the result of structure-based design and proved to be potent DHODH inhibitors which in addition showed good antiproliferative activities on peripheral blood mononuclear cells and good efficacies in vivo in the rat adjuvant-induced-arthritis model.

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