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
Full Text: HTML
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.
Related Articles:
Development of trityl-based photolabile hydroxyl protecting groups
[Zhou, Lei; Yang, Haishen; Wang, Pengfei Journal of Organic Chemistry, 2011 , vol. 76, # 15 p. 5873 - 5881]
Mizoroki–Heck Reactions with 4??Phenoldiazonium Salts
[Schmidt, Bernd; Hoelter, Frank; Berger, Rene; Jessel, Soenke Advanced Synthesis and Catalysis, 2010 , vol. 352, # 14-15 p. 2463 - 2473]