Tyrphostins. II. Heterocyclic and. alpha.-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases

A Gazit, N Osherov, I Posner, P Yaish…

Index: Gazit, Aviv; Osherov, Nir; Posner, Israel; Yaish, Pnina; Poradosu, Enrique; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 6 p. 1896 - 1907

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Citation Number: 256

Abstract

We have previously described a novel series of low molecular weight protein tyrosine kinase inhibitors which we named tyrphostins. The characteristic active pharmacophore of these compounds was the hydroxy-cisbenzylidenemalononitrile moiety. In this article we describe three novel groups of tyrphostins:(i) one group has the phenolic moiety of the cis- benzylidenemalononitrile replaced either with other substituted benzenes or with ...