158365-54-9Relevant academic research and scientific papers
Preparation and Binding Affinity of New Porphyrin Host Molecule for Ubiquinone Analogues
Hayashi, Takashi,Miyahara, Takashi,Aoyama, Yasunori,Nonoguchi, Masanori,Ogoshi, Hisanobu
, p. 1749 - 1752 (1994)
αααα-meso-Tetra(7-hydroxy-1-naphthyl)porphyrin (1) is prepared as a host molecule for ubiquinone analogue, 2,3,5,6-tetramethoxy-p-benzoquinone (2).The affinity and thermodynamic aspects in porphyrin 1 - quinone 2 pairing were determined by titrimetric measyrement of electronic absorption and fluorescence spectra.The binding constant of 1 for 2 at 298 K is obtained; Ka = 7.9*102 M-1 in toluene.The fashion of this porphyrin-quinone pairing was large different from that of previous host, αααα-meso-tetra(2-hydroxy-1-naphthyl)porphyrin (3), - quinone 2 pairing.
A high-affinity subtype-selective fluorescent probe for estrogen receptor β imaging in living cells
Hu, Zhiye,Yang, Lu,Ning, Wentao,Tang, Chu,Meng, Qiuyu,Zheng, Jie,Dong, Chune,Zhou, Hai-Bing
, p. 3887 - 3890 (2018)
Estrogen receptor β (ERβ) has recently been identified as a pharmaceutical target in hormone replacement therapy for breast cancers. However, the biological function of ERβ in disease progression remains unclear. A highly ERβ-selective fluorescent probe (
A facile synthesis of melatonergic antidepressant agomelatine
Kandagatla, Bhaskar,Raju, Vetukuri Venkata Naga Kali Vara Prasada,Reddy, Ganta Madhusudhan,Rao, Sirigiri Chandrakanth,Iqbal, Javed,Bandichhor, Rakeshwar,Oruganti, Srinivas
, p. 7125 - 7127 (2013/01/15)
Agomelatine was synthesized from 8-aminonaphthalen-2-ol by diazotization-iodination, formylation, C-C bond formation by nitroaldol and Pd/C hydrogenation of β-nitrovinylnaphthalene followed by N-acetylation. The route reported employs readily and commercially viable starting materials and reagents, and can potentially be utilized for process synthesis of agomelatine.
17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS FOR THE TREATMENT OF HORMONE-RELATED DISEASES
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Page/Page column 14, (2010/08/18)
The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases.The invention further relates to suitable inhibitors and to a method for the production thereof.
ERβ ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERβ selectivity
Mewshaw, Richard E.,Edsall Jr., Richard J.,Yang, Cuijian,Manas, Eric S.,Xu, Zhang B.,Henderson, Ruth A.,Keith Jr., James C.,Harris, Heather A.
, p. 3953 - 3979 (2007/10/03)
The 2-phenylnaphthalene scaffold was explored as a simplified version of genistein in order to identify ER selective ligands. With the aid of docking studies, positions 1, 4, and 8 of the 2-phenylnaphthalene template were predicted to be the most potentially influential positions to enhance ER selectivity using two different binding orientations. Both orientations have the phenol moiety mimicking the A-ring of genistein. Several compounds predicted to adopt orientations similar to that of genistein when bound to ERβ were observed to have slightly higher ER affinity and selectivity than genistein. The second orientation we exploited, which was different from that of genistein when bound to ERβ, resulted in the discovery of several compounds that had superior ER selectivity and affinity versus genistein. X-ray structures of two ER selective compounds (i.e., 15 and 47) confirmed the alternate binding mode and suggested that substituents at positions 1 and 8 were responsible for inducing selectivity. One compound (i.e., 47, WAY-202196) was further examined and found to be effective in two models of inflammation, suggesting that targeting ER may be therapeutically useful in treating certain chronic inflammatory diseases.
Process for the synthesis of 3-(3-fluoro-4-hydroxyphenyl)-7-hydroxynaphthonitrile
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Page/Page column 3-4; 7, (2008/06/13)
A process for making a compound of formula I and intermediate compounds thereof, wherein R1 is CN, F or Cl; R2 is H or Br; and R3 and R4 are each independently H or F. The compounds of formula I are useful in th
Substituted phenyl naphthalenes as estrogenic agents
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, (2008/06/13)
This invention provides estrogen receptor modulators of formula I, having the structure 1wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10, are as defined in the specification, or a pharmaceutically acceptable salt thereof.
Photoexcited proton transfer from enhanced photoacids
Tolbert, Laren M.,Haubrich, Jeanne E.
, p. 10593 - 10600 (2007/10/02)
Naphthols with electron-withdrawing groups such as cyano or methanesulfonyl at C-5 and C-8 exhibit greatly enhanced photoacidity. This increase in photoacidity enables the substituted naphthols to undergo excited-state proton transfer (ESPT) in alcohols and Me2SO in the absence of water. In aqueous tetrahydrofuran solution, efficient proton transfer to water occurs at much lower water concentrations than with the parent naphthol, and the kinetics of proton transfer indicate that a smaller water cluster is involved.
