1007126-06-8Relevant academic research and scientific papers
Novel 8-arylated purines as inhibitors of glycogen synthase kinase
Ibrahim, Nada,Mouawad, Liliane,Legraverend, Michel
scheme or table, p. 3389 - 3393 (2010/08/06)
A series of 8-arylated purine derivatives bearing either an aniline or an alkyl amide at position 6 were found to inhibit glycogen synthase kinase-3,with good selectivity over ten kinases. Molecular modeling studies indicated that the most active compounds (8a and 8e),adopt a planar conformation,close to the shape of AMPPNP in the crystal structure of GSK-3. These compounds are stabilized by hydrophobic contacts between the 8-aromatic group and the protein adenine pocket and by electrostatic contacts.
Heteroaryl compounds useful as inhibitors of E1 activating enzymes
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Page/Page column 114, (2008/06/13)
This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
