Biaryl analogues of teriflunomide as potent DHODH inhibitors

…, P Pizcueta, N Godessart, JC Castro-Palomino

Index: Erra, Montse; Moreno, Imma; Sanahuja, Jordi; Andres, Miriam; Reinoso, Raquel F.; Lozoya, Estrella; Pizcueta, Pilar; Godessart, Nuria; Castro-Palomino, Julio Cesar Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 24 p. 7268 - 7272

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Citation Number: 8

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.