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

Novel diphenylamine-type estrogen receptor ligands were designed and synthesized, and their biological activities were evaluated by means of binding assays for estrogen receptor-α and -β 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.

Graphical abstractNovel diphenylamine-type estrogen receptor ligands were designed and synthesized, and showed moderate estrogenic activities. We propose that the diphenylamine skeleton may be a privileged core structure for various nuclear receptor ligands.Figure optionsDownload full-size imageDownload as PowerPoint slide