Nantogmah, S. published the artcileSynthesis and preliminary evaluation of affinity to retinoic acid receptors for new organosilicon-based retinoids, Application In Synthesis of 50670-76-3, the publication is Pharmaceutical Chemistry Journal (2012), 45(10), 612-621, database is CAplus.
Two facile synthetic routes to eleven new Si-containing ligands for retinoic acid receptors (RARs) are reported. The design of these RAR ligands is based on a pharmacophoric model that divides the mols. into three regions that are necessary for efficient binding to the corresponding receptors: a hydrophobic region (A), a linker or tether region (B) and a hydrophilic region (C). The ligands are unique in region A due to their acyclic nature and the presence of alkyl-substituted Si at the core. The substituted silyl groups were used to fulfill pharmacophore requirements. Various alkyl substituents available on the Si starting materials afford an opportunity to explore steric effects on binding. In region B of four ligands, a cinnamate moiety maintains some degree of conjugation and planarity in the mols. A biaryl group used in region B of another series of compounds is known to lead to RARb selectivity. Finally, region C of the ligands contains a carboxylate group, a well known pharmacophore requirement for RAR ligands. The compounds prepared in this work have micromolar to nanomolar affinity for these medically relevant target receptors. The proposed silane-containing ligands represent siloacetylenic aryl acids that are worth of further study. They may serve as leads for the development of higher-affinity, more receptor-selective agents.
Pharmaceutical Chemistry Journal published new progress about 50670-76-3. 50670-76-3 belongs to esters-buliding-blocks, auxiliary class Benzene,Phenol,Ester, name is Ethyl 4′-hydroxy-[1,1′-biphenyl]-4-carboxylate, and the molecular formula is C15H14O3, Application In Synthesis of 50670-76-3.
Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics