Synthesis and characterization of a new RXR agonist based on the 6-tert-butyl-1,1-dimethylindanyl structure.
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.
Domínguez
Beatriz
B
Departamento de Qui;mica Orgánica, Facultad de Ciencias, Universidade de Vigo, 36200, Vigo, Spain.
Vega
M Jesús
MJ
Sussman
Fredy
F
de Lera
Angel R
AR
D002073:Butanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007189:Indans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008958:Models, Molecular; D015394:Molecular Structure; D018168:Receptors, Retinoic Acid / Q000819:agonists*; D047488:Retinoid X Receptors; D014157:Transcription Factors / Q000819:agonists*
C470972:6-tert-butyl-1,1-dimethylindanyl; D002073:Butanes; D007189:Indans; D018168:Receptors, Retinoic Acid; D047488:Retinoid X Receptors; D014157:Transcription Factors