43024-66-4Relevant academic research and scientific papers
INHIBITORS OF AKT ACTIVITY
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Page/Page column 131-132, (2010/10/03)
The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
Synthesis of new pyrazolo[1,5-a]pyrimidines and pyrazolo[3,4-b]pyridines
Al-Mousawi,Mohammad,Elnagdi
, p. 989 - 991 (2007/10/03)
While 3(5)-aminopyrazole reacts with enaminonitrile to yield pyrazolo[1,5-a]pyrimidines, 3-amino-5-pyrazolone reacts with the same reagents to yields pyrazolo[3,4-b]pyridines.
Synthesis and Enzymic Activity of 6-Carbethoxy- and 6-Ethoxy-3,7-disubstituted-pyrazolopyrimidines and Related Derivatives as Adenosine Cyclic 3',5'-Phosphate Phosphodiesterase Inhibitors
Springer, Robert H.,Scholten, M. B.,O'Brien, Darrell E.,Novinson, Thomas,Miller, Jon P.,Robins, Roland K.
, p. 235 - 242 (2007/10/02)
A number of 3,7-disubstituted 6-carbethoxypyrazolopyrimidines and 3,7-disubstituted 6-ethoxypyrazolopyrimidines have been prepared and evaluated as adenosine cyclic 3',5'-phosphate (cAMP) phosphodiesterase (PDE) inhibitors vs. the low Km enzyme isolated from beef heart, rabbit lung, and kidney preparations.The results were found to be between 0.5 to 13 times as potent as theophylline as inhibitors of PDE, depending on the tissue source.A number of these PDE inhibitors exhibited significant physiological effects in different animal systems, suggesting it should be possible to obtain selective PDE inhibition in various tissues.Several of these heterocycles were found superior to adenosine in inhibiting ADP-induced platelet aggregation in vitro.
