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growth of humanbreast carcinoma MCF-7transplanted in nude mice5). However, it is unstable and easily degraded in serum6) and in cell culture medium (K. Umezawa; unpublished results). Therefore, we synthesized methyl 2,5-dihydroxycinnamate (2,5-MeC) as a stable analogue of erbstatin3). It inhibited EGF-induced S-phase entry3), cellular src functions4), and in vivo growth of MCF-7tumors (Dr. M. Toi, Hiroshima University; personal communication) more prominently than erbstatin. In this presently reported study we synthesized several new alkyl dihydroxycinnamates and an aldehyde derivative as more stable analogues of erbstatin and examined their inhibitory activity on tyrosine kinase and cellular src oncogene functions. We synthesized alkyl 2,5-dihydroxycinnamates7)

Inhibition of tyrosine kinase and src oncogene functions by stable erbstatin analogues.