silicon has been researched along with tamibarotene* in 2 studies
2 other study(ies) available for silicon and tamibarotene
| Article | Year |
|---|---|
Structural Development of Silicon-Containing Retinoids: Structure-Activity Relationship Study of the Hydrophobic Pharmacophore of Retinobenzoic Acids Using Silyl Functionalities.
We designed and synthesized a series of retinobenzoic acids bearing various silyl functionalities in order to explore in detail the structure-activity relationship (SAR) at the hydrophobic moiety of retinoids. Among the synthesized compounds, 24 c bearing a t-butyldimethylsilyl (TBS) group at the hydrophobic site exhibited potent retinoid activity comparable to that of the lead compound Am555S (4). Compound 24 c exhibited transcription-promoting activity towards all three subtypes of retinoic acid receptor (RAR), but showed the highest activity towards RARγ, in contrast to the high RARα-selectivity of Am80 (3) and Am555S (4). The SARs presented here should be helpful in the development of subtype-selective retinoids, and in particular 24 c might be a promising lead compound for new RARγ ligands. Topics: Benzoates; Retinoid X Receptors; Retinoids; Silicon; Structure-Activity Relationship; Tetrahydronaphthalenes; Tretinoin | 2022 |
Synthesis and pharmacological characterization of Disila-AM80 (Disila-tamibarotene) and Disila-AM580, silicon analogues of the RARalpha-selective retinoid agonists AM80 (Tamibarotene) and AM580.
Topics: Antineoplastic Agents; Benzoates; HeLa Cells; Humans; Organosilicon Compounds; Phthalic Acids; Receptors, Retinoic Acid; Retinoic Acid Receptor alpha; Silicon; Tetrahydronaphthalenes | 2009 |