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

K Ohta, Y Chiba, T Ogawa, Y Endo

Index: Ohta, Kiminori; Chiba, Yuki; Ogawa, Takumi; Endo, Yasuyuki Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 18 p. 5050 - 5053

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Citation Number: 30

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-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 ...