Synthesis and characterization of a new RXR agonist based on the 6-tert-butyl-1,1-dimethylindanyl structure.

Article Details

Citation

Copy to clipboard

Dominguez B, Vega MJ, Sussman F, de Lera AR

Synthesis and characterization of a new RXR agonist based on the 6-tert-butyl-1,1-dimethylindanyl structure.

Bioorg Med Chem Lett. 2002 Sep 16;12(18):2607-9.

PubMed ID

12182871 [ View in PubMed

]

Abstract

A new ligand for RXR is described, which is based on a 6-tert-butyl-1,1-dimethylindanyl skeleton as bioisostere of the hydrophobic retinoid region. The Stille cross-coupling reaction allowed the attachment of the polyene side chain to the indanyl ring. Docking studies were carried out to explain the RXR binding profile of this analogue.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Bexarotene	Retinoic acid receptor RXR-alpha	Kd (nM)	36	N/A	N/A	Details
Tretinoin	Retinoic acid receptor RXR-alpha	Kd (nM)	50	N/A	N/A	Details