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

Article Details

Citation

Copy to clipboard

Ohta K, Chiba Y, Ogawa T, Endo Y

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. Epub 2008 Aug 6.

PubMed ID

18760603 [ View in PubMed

]

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Estradiol	Estrogen receptor alpha	IC 50 (nM)	4	N/A	N/A	Details
Estradiol	Estrogen receptor beta	IC 50 (nM)	4	N/A	N/A	Details