Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors

A Gazit, P Yaish, C Gilon, A Levitzki

Index: Gazit, Aviv; Yaish, Pnina; Gilon, Chaim; Levitzki, Alexander Journal of Medicinal Chemistry, 1989 , vol. 32, # 10 p. 2344 - 2352

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Citation Number: 596

Abstract

A novel class of low molecular weight protein tyrosine kinase inhibitors is described. These compounds constitute a systematic series of molecules with a progressive increase in affinity toward the substrate site of the EGF receptor kinase domain. These competitive inhibitors also effectively block the EGF-dependent autophosphorylation of the receptor. The potent EGF receptor kinase blockers examined were found to competitively inhibit the ...