Novel retinoic acid receptor alpha agonists: syntheses and evaluation of pyrazole derivatives.
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 RAR alpha receptor, and had highly potent cell-differentiating activity on HL-60 cells.
Kikuchi
K
K
Tsukuba Basic Research Laboratories for Drug Discovery, Eisai Co. Ltd., Ibaraki, Japan.
Hibi
S
S
Yoshimura
H
H
Tai
K
K
Hida
T
T
Tokuhara
N
N
Yamauchi
T
T
Nagai
M
M
D001667:Binding, Competitive; D002454:Cell Differentiation / Q000187:drug effects; D018922:HL-60 Cells; D006801:Humans; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018168:Receptors, Retinoic Acid / Q000819:agonists*; D000072482:Retinoic Acid Receptor alpha; D013329:Structure-Activity Relationship
D011720:Pyrazoles; C000607071:RARA protein, human; D018168:Receptors, Retinoic Acid; D000072482:Retinoic Acid Receptor alpha