Thiophene-Core Estrogen Receptor Ligands Having Superagonist Activity
摘要:
To probe the importance of the heterocyclic core of estrogen receptor (ER) ligands, we prepared a series of thiophene-core ligands by Suzuki cross coupling of aryl boronic acids with bromo-thiophenes and we assessed their receptor binding and cell biological activities. The disposition of the phenol substituents on the thiophene core, at alternate or adjacent sites, and the nature of substituents on these phenols, all contribute to binding affinity and subtype selective. Most of the bis(hydroxyphenyl)-thiophenes were ER beta selective, whereas the tris(hydroxyphenyl)-thiophenese were ER alpha selective; analogous furan-core compounds generally have lower affinity and less selectivity. Some diarylthiophenes show distinct superagonist activity, in reporter gene assays, giving maximal activities 2-3 times that of estradiol, and modeling suggests that these ligands have a different interaction with a hydrogen-bonding residue in helix-11 Ligand-core modification may be a new strategy for developing ER ligands whose selectivity is based on having transcriptional activity greater than that of estradiol.
A novel porphyrin-based porous organic polymer PPOP-1(Pd) with bifunctional catalytic sites was constructed via imine condensation of tetra(4-aminophenyl)porphyrin and acenaphthenequinone. PPOP-1(Pd) containing Pd(II)-porphyrin and Pd(II)-α-diimine moieties exhibits excellent catalytic activity and outstanding reusability for tandem catalytic reactions of C–H arylation and Suzuki coupling.
Kao et al., Proceedings - Indian Academy of Sciences, Section A, 1950, # 32, p. 162,166
作者:Kao et al.
DOI:——
日期:——
POLYMERIZABLE COMPOUND HAVING OXYGEN-CONTAINING FIVE-MEMBERED RING, LIQUID CRYSTAL COMPOSITION AND LIQUID CRYSTAL DISPLAY DEVICE
申请人:JNC CORPORATION
公开号:US20150034871A1
公开(公告)日:2015-02-05
An object is to provide a polymerizable compound having high polymerization reactivity, a high conversion ratio and high solubility in a liquid crystal composition, a polymerizable composition containing the compound, a liquid crystal composite prepared from the composition, and a liquid crystal display device having the composite. A solution is a polymerizable compound represented by formula (1).
In the formula, for example, P
1
and P
2
are —OCO—(CH
3
)C═CH
2
; S
1
and S
2
are a single bond; ring A
1
, ring A
2
and ring A
3
are 1,4-phenylene; Z
1
, Z
2
and Z
3
are a single bond; two of G is —CH═ or —N═; and a is 0 or 1.