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Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties by Fabrice Pierre; Sean E. O’Brien; Mustapha Haddach; Pauline Bourbon; Michael K. Schwaebe; Eric Stefan; Levan Darjania; Ryan Stansfield; Caroline Ho; Adam Siddiqui-Jain; Nicole Streiner; William G. Rice; Kenna Anderes; David M. Ryckman is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties about?

We describe the discovery of novel potent substituted pyrimido [4,5-c]quinoline ATP-competitive inhibitors of protein kinase CK2. A binding model of the inhibitors with the protein was elaborated on the basis of SAR and revealed various modes of interaction with the hinge region. Representative analog 14k (CK2 IC 50 = 9 nM) showed anti-viral activity at nanomolar concentrations against HIV-1. Orally available compound 7e (CK2 IC 50 = 3 nM) reduced pain in the phase II of a murine formalin model. These preliminary data confirm that properly optimized CK2 inhibitors may be used for anti-viral and pain therapy.

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Author

Fabrice Pierre; Sean E. O’Brien; Mustapha Haddach; Pauline Bourbon; Michael K. Schwaebe; Eric Stefan; Levan Darjania; Ryan Stansfield; Caroline Ho; Adam Siddiqui-Jain; Nicole Streiner; William G. Rice; Kenna Anderes; David M. Ryckman

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)

Published

2011

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)