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ID: ALA1133434

Journal: Bioorg Med Chem Lett

Title: Novel retinoic acid receptor alpha agonists: syntheses and evaluation of pyrazole derivatives.

Authors: Kikuchi K, Hibi S, Yoshimura H, Tai K, Hida T, Tokuhara N, Yamauchi T, Nagai M.

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 RAR alpha receptor, and had highly potent cell-differentiating activity on HL-60 cells.

CiteXplore: 10762038

DOI: 10.1016/s0960-894x(00)00066-4