1016161-79-7Relevant academic research and scientific papers
Formation of a Cubic Liquid Crystalline Nanostructure with π-Conjugated Fluorinated Rods on the Gyroid Minimal Surface
Poppe, Marco,Chen, Changlong,Liu, Feng,Poppe, Silvio,Tschierske, Carsten
, p. 7196 - 7200 (2017)
Bicontinuous cubic phases are of significant importance for numerous applications, for example, for the crystallization of membrane proteins, as photonic materials and as templates for porous silica. A new variant of bicontinuous cubic liquid crystalline
Investigating 3,3-diaryloxetanes as potential bioisosteres through matched molecular pair analysis
Bull, James A.,Choi, Chulho,Croft, Rosemary A.,Ding, Yujie,Dubois, Maryne A. J.,Mousseau, James J.,Owen, Dafydd R.
supporting information, p. 2045 - 2052 (2022/02/23)
Oxetanes have received increasing interest in medicinal chemistry as attractive polar and low molecular weight motifs. The application of oxetanes as replacements for methylene, methyl,gem-dimethyl and carbonyl groups has been demonstrated to often improve chemical properties of target molecules for drug discovery purposes. The investigation of the properties of 3,3-diaryloxetanes, particularly of interest as a benzophenone replacement, remains largely unexplored. With recent synthetic advances in accessing this motif we studied the effects of 3,3-diaryloxetanes on the physicochemical properties of ‘drug-like’ molecules. Here, we describe our efforts in the design and synthesis of a range of drug-like compounds for matched molecular pair analysis to investigate the viability of the 3,3-diaryloxetane motif as a replacement group in drug discovery. We conclude that the properties of the diaryloxetanes and ketones are similar, and generally superior to related alkyl linkers, and that diaryloxetanes provide a potentially useful new design element.
Characterization of thyroid hormone receptor α (TRα)-specific analogs with varying inner- and outer-ring substituents
Ocasio, Cory A.,Scanlan, Thomas S.
, p. 762 - 770 (2008/09/17)
Analogs of the TRα-specific thyromimetic CO23 were synthesized and analyzed in vitro using competitive binding and transactivation assays. Like CO23, all analogs bind to both thyroid hormone receptor subtypes with about the same affinity; however, modification of CO23 by derivatization of the 3′ position of the outer-ring or replacement of the inner-ring iodides with bromides attenuates binding. Despite lacking a preference in binding to TRα, all analogs display TRα-specificity in transactivation assays using U2OS and HeLa cells. At best, several agonists exhibit an approximately 6-12-fold preference in transactivation when tested with TRα in HeLa cells. One analog, CO24, showed in vivo TRα-specific action in a tadpole metamorphosis assay.
