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Nitrostyrene Derivatives of Adenosine 5′-Glutarates as Selective Inhibitors of the Epidermal Growth Factor Receptor Protein Tyrosine Kinase

✍ Scribed by Stefan Peterli; Regina Stumpf; Marc Schweizer; Urs Séquin; Helmut Mett; Peter Traxler

Publisher
John Wiley and Sons
Year
1992
Tongue
German
Weight
751 KB
Volume
75
Category
Article
ISSN
0018-019X

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✦ Synopsis

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 IC~50~ 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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## Synthesis of Modified Tripeptides and Tetrapeptides as Potential Bisubstrate Inhibitors of the Epidermal Growth Factor Receptor Protein Tyrosine Kinase. -Compound (Ia) is the best bisubstrate-type inhibitor among the three peptides synthesized.