Nitrostyrene Derivatives of Adenosine 5′-Glutarates as Selective Inhibitors of the Epidermal Growth Factor Receptor Protein Tyrosine Kinase |
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Authors: | Stefan Peterli Regina Stumpf Marc Schweizer Urs Squin Helmut Mett Peter Traxler |
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Institution: | Stefan Peterli,Regina Stumpf,Marc Schweizer,Urs Séquin,Helmut Mett,Peter Traxler |
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Abstract: | The syntheses and biological activities of some nitrostyrene derivatives of adenosine 5′-glutarates, a novel class of selective, bi-substrate-type inhibitors of the EGF receptor protein tyrosine kinase with IC50 values around 1 μM . Only marginal inhibition of the tyrosine kinases v-able and c-src and of the serine/threonine kinase PKC was observed. Compounds 8, 9, 11 , and 12 – lacking the adenosine moiety – were ten times less active than the most potent derivatives, whereas 17 – lacking the nitrostyryl part – showed no inhibitory activity at all. Most of the compounds showed potent antiproliferative activity against an EGF-dependent mouse keratinocyte cell line. |
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