Promising core structure for nuclear receptor ligands: design and synthesis of novel estrogen receptor ligands based on diphenylamine skeleton

  • Bioorg Med Chem Lett. 2008 Sep 15;18(18):5050-3. doi: 10.1016/j.bmcl.2008.08.004.
Kiminori Ohta  1 ,  Yuki Chiba ,  Takumi Ogawa ,  Yasuyuki Endo
Affiliations
  • 1. Faculty of Pharmaceutical Sciences, Tohoku Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai 981-8558, Japan.
PMID: 18760603 DOI: 10.1016/j.bmcl.2008.08.004
Abstract

Novel diphenylamine-type Estrogen receptor ligands were designed and synthesized, and their biological activities were evaluated by means of binding assays for estrogen receptor-alpha and -beta and cell proliferation assay using MCF-7 cells. Compounds 4f, 11b, 12c, and 8 showed moderate estrogenic activities. We propose that the diphenylamine skeleton may be a privileged structure for various nuclear receptor ligands, including RAR, RXR, and AR ligands.

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