Author/Authors :
Kouichi Kikuchi، نويسنده , , Shigeki Hibi، نويسنده , , Hiroyuki Yoshimura، نويسنده , , Kenji Tai، نويسنده , , Takayuki Hida، نويسنده , , Naoki Tokuhara، نويسنده , , Toshihiko Yamauchi، نويسنده , , Mitsuo Nagai، نويسنده ,
Abstract :
We have designed and synthesized a series of pyrazole derivatives as candidate retinoic acid receptor (RAR) agonists. One of them, 4-[5-(1, 5-diisopropyl-1H-3-pyrazolyl)-1H-2-pyrrolyl]benzoic acid (11b), which possesses a 2,5-disubstituted pyrrole moiety, showed selective transactivation activity for the RARα receptor, and had highly potent cell-differentiating activity on HL-60 cells.