Discovering a new analogue of thalidomide which may be used as a potent modulator of TNF-alpha production.
A new series of imide derivatives related to thalidomide were synthesized and evaluated as modulators of TNF-alpha production. These derivatives enhance TNF-alpha production using human leukemia HL-60 cells induced with 12-O-tetradecanoylphorbol 13-acetate (TPA), while inhibiting TNF-alpha production induced with okadaic acid (OA) in the same cell line. The diphenylmaleimide derivative 2f, was found to be the most active product, producing a strong modulation of the cytokine level.
Fernández Braña
Miguel
M
Instituto Canario de Investigación del Cáncer, Brasil 25, 28110 Algete, Madrid, Spain. mifbrana@gmail.com
Acero
Nuria
N
Añorbe
Loreto
L
Muñoz Mingarro
Dolores
D
Llinares
Francisco
F
Domínguez
Gema
G
D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D007938:Leukemia / Q000188:drug therapy / Q000378:metabolism; D013792:Thalidomide / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism*
D014409:Tumor Necrosis Factor-alpha; D013792:Thalidomide