186970-32-1Relevant academic research and scientific papers
MOLECULAR PROBE PRECURSOR FOR PANCREATIC ISLET IMAGING AND USE OF SAME
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, (2012/02/04)
A precursor of a molecular probe for imaging of pancreatic islets is a compound expressed as the following formula (I): wherein -V-X represents a substituent on a benzene ring, V represents a bond, R1, or OR1, R1 represent
NOVEL ANTIDIABETIC COMPOUNDS
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Page/Page column 77-78, (2010/11/29)
The present invention provides novel compounds of the general formula (I), wherein the symbols are same as described in specification, their pharmaceutically acceptable salts, their tautomeric forms, their stereoisomers, pharmaceutical compositions containing them, to process and intermediates for the preparation of the above said compounds, having the utility of these compounds in medicine and to methods for their therapeutic use, and their use in the treatment of diabetes and related diseases.
1-Aryl-2-pyridyl-3,4-dihydronaphthalenes: Photofluorogenic ligands for the estrogen receptor
Scribner, Andrew W.,Haroutounian, Serkos A.,Carlson, Kathryn E.,Katzenellenbogen, John A.
, p. 1043 - 1057 (2007/10/03)
Three 1,2-substituted-3,4-dihydronaphthalenes that are pyridine analogs of the antiestrogen desmethylnafoxidine were prepared and evaluated as fluorescent ligands for the estrogen receptor. These compounds represent a class of fluorescent probes that we term 'photofluorogenic', denoting their ability to exist initially as a high affinity though weakly fluorescent stilbazole form which can be photocyclized-oxidized to a highly fluorescent though low affinity azaphenanthrenoid form. These probes also contain an aziridine function that provides a means for their permanent, covalent attachment to the receptor. The three dihydronaphthalene systems were prepared by efficient routes from α-(2-, 3-, and 4-pyridyl)acetophenone precursors. They demonstrate high apparent affinity for the estrogen receptor and show time-dependent irreversible inactivation, consistent with their covalent attachment to the receptor via the aziridine function. Each system is converted into an azaphenanthrene by photocyclization-oxidation of the cis-stilbazole unit. The absorbance and fluorescence emission spectra of the dihydronaphthalene precursors and azaphenanthrene products have been characterized, and they display marked sensitivity to both solvent polarity and pH. The azaphenanthrenoids derived from the 2- and 4-pyridyl isomers exhibit intense emission at wavelengths that exceed 500 nm under certain conditions and appear to be well suited as fluorescent probes for the estrogen receptor.
