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

Beatriz Domínguez; M Jesús Vega; Fredy Sussman; Angel R de Lera

doi:10.1016/s0960-894x(02)00477-8

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. doi: 10.1016/s0960-894x(02)00477-8.

Authors

Beatriz Domínguez¹, M Jesús Vega, Fredy Sussman, Angel R de Lera

Affiliation

¹ Departamento de Qui;mica Orgánica, Facultad de Ciencias, Universidade de Vigo, 36200, Vigo, Spain.

PMID: 12182871
DOI: 10.1016/s0960-894x(02)00477-8

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Butanes / chemical synthesis*
Butanes / chemistry
Butanes / pharmacology
Indans / chemical synthesis*
Indans / chemistry
Indans / pharmacology
Models, Molecular
Molecular Structure
Receptors, Retinoic Acid / agonists*
Retinoid X Receptors
Transcription Factors / agonists*

Substances

6-tert-butyl-1,1-dimethylindanyl
Butanes
Indans
Receptors, Retinoic Acid
Retinoid X Receptors
Transcription Factors