203115-86-0Relevant academic research and scientific papers
Green traceless cleavage from resin-bound selenium and tellurium and analysis by 2D29Si/1H HR-MAS NMR spectroscopy
Ruhland, Thomas,Torang, Jakob,Pedersen, Henrik,Madsen, Jens Christian,Bang, Kia Svane
, p. 1635 - 1640 (2005)
A novel protocol for traceless cleavage from resin-bound selenium and tellurium is described. The toxic tributyltin hydride that has been used previously as reagent for cleavage from these resins by homolysis has been replaced by the less-toxic tris(trime
Selenium-linking strategy for traceless solid-phase synthesis: Direct loading, aliphatic C-H bond formation upon cleavage and reaction monitoring by gradient MAS NMR spectroscopy
Ruhland, Thomas,Andersen, Kim,Pedersen, Henrik
, p. 9204 - 9211 (1998)
The development of a novel traceless linking strategy for the solid- phase synthesis of small non- peptide compounds by the use of resin-bound selenium is described. Compounds were attached by direct loading without the requirement of an auxiliary spacer.
Traceless solid phase synthesis with polystyrene-bound tellurium and in comparison with polystyrene-bound selenium
Ruhland, Thomas,Torang, Jakob,Pedersen, Henrik,Madsen, Jens Christian,Bang, Kia Svane
, p. 2323 - 2328 (2004)
A novel traceless linking strategy by use of polystyrene-bound tellurium is described. The application of the tellurium linker is demonstrated by the solid phase synthesis of a small library of single alkyl aryl ethers containing two points of diversity.
Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors
Jong, Yeon Hwang,Arnold, Leggy A.,Zhu, Fangyi,Kosinski, Aaron,Mangano, Thomas J.,Setola, Vincent,Roth, Bryan L.,Guy, R. Kiplin
supporting information; experimental part, p. 3892 - 3901 (2010/02/17)
We have previously reported the discovery and preliminary structure activity relationships of a series of β-aminoketones that disrupt the binding of coactivators to TR. However, the most active compounds had moderate inhibitory potency and relatively high cytotoxicity, resulting in narrow therapeutic index. Additionally, preliminary evaluation of in vivo toxicology revealed a significant dose related cardiotoxicity. Here we describe the improvement of pharmacological properties of thyroid hormone receptor coactivator binding inhibitors. A comprehensive survey of the effects of substitutents in key areas of the molecule was carried out based on mechanistic insight from the earlier report. This study revealed that both electron withdrawing and hydrophobic substituents on the aromatic ring led to higher potency. On the other hand, moving from an alkyl to a sulfonyl alkyl side chain led to reduced cytotoxicity. Finally, utilization of amine moieties having low pKa's resulted in lowered ion channel activity without any loss of pharmacological activity.
Synthesis and thermal properties for 4-(4-alkoxyphenoxycarbonyl)phenyl 3-alkoxy-2-X-benzoates
Okamoto, Hiroaki,Morita, Yuki,Segawa, Yoichi,Takenaka, Shunsuke
, p. 221/[2087]-227/[2093] (2007/10/03)
Some derivatives of 4-(4-alkoxyphenoxycarbonyl)phenyl 3-alkoxy-2-X- benzoates (X=F, Cl, Br, or CF3) were synthesized by means of an ortho-directed lithiation followed by an electrophilic aromatic substitution reaction, as a key step, and their
