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, are described. The most interesting compounds (14-16) were able to inhibit the EGF-R tyrosine kinase with IC,, values around 1 p~. Only marginal inhibition of the tyrosine kinases u-ubl 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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