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.
Departamento de Qui;mica Orgánica, Facultad de Ciencias, Universidade de Vigo, 36200, Vigo, Spain.
Beatriz
B
Domínguez
M Jesús
MJ
Vega
Fredy
F
Sussman
Angel R
AR
de Lera
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