New potent and selective A1 adenosine receptor antagonists as potential tools for the treatment of gastrointestinal diseases
The synthesis of 9-alkyl substituted adenine derivatives presenting aromatic groups and cycloalkyl rings in 8- and N6-position, respectively, is reported. The compounds were tested with radioligand binding studies showing, in some cases, a low
Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors
On the basis of ATP adenine, a series of adenine and purine derivatives was prepared and tested for their ability to inhibit a spectrum of disease-related kinases. There has been scant research investigating the potential of cosubstrate derived kinase inhibitors for other kinases than CDKs. Our inhibitor design combined the purine system from the original cosubstrate ATP and phenyl moieties in order to explore possible interactions with the different regions of the ATP binding site in several disease-related protein kinases. There have been a number of hits for the assayed substances, which led us to conclude that the spectrum of compounds may prove to be a valuable tool kit for the evaluation of bonding and selectivity patterns for a wide variety of kinases.
Laufer, Stefan A.,Domeyer, David M.,Scior, Thomas R. F.,Albrecht, Wolfgang,Hauser, Dominik R. J.
p. 710 - 722
(2007/10/03)
A1 adenosine receptor antagonists
Disclosed are A1adenosine receptor antagonists, useful for treating various disease states, in particular disease states for which diuretic treatment is appropriate.
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Page/Page column 9
(2008/06/13)
The reaction of 6-halopurines with phenyl metal complexes
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McKenzie,Glass
p. 1551 - 1553
(2007/10/02)
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