1582776-44-0Relevant articles and documents
Dual RXR agonists and RAR antagonists based on the stilbene retinoid scaffold
Martínez, Claudio,Lieb, Michele,álvarez, Susana,Rodríguez-Barrios, Fátima,álvarez, Rosana,Khanwalkar, Harshal,Gronemeyer, Hinrich,De Lera, Angel R.
, p. 533 - 537 (2014/06/09)
Arotinoids containing a C5,C8-diphenylnaphthalene-2-yl ring linked to a (C3-halogenated) benzoic acid via an ethenyl connector (but not the corresponding naphthamides), which are prepared by Horner-Wadsworth-Emmons reaction of naphthaldehydes and benzylphosphonates, display the rather unusual property of being RXR agonists (15-fold induction of the RXR reporter cell line was achieved at 3- to 10-fold lower concentration than 9-cis-retinoic acid) and RAR antagonists as shown by transient transactivation studies. The binding of such bulky ligands suggests that the RXR ligand-binding domain is endowed with some degree of structural elasticity.