Structure-activity relationships in a series of 5-[(2, 5-dihydroxybenzyl) amino] salicylate inhibitors of EGF-receptor-associated tyrosine kinase: importance of additional …

H Chen, J Boiziau, F Parker, P Mailliet…

Index: Chen; Boiziau; Parker; Mailliet; Commercon; Tocque; Le Pecq; Roques; Garbay Journal of Medicinal Chemistry, 1994 , vol. 37, # 6 p. 845 - 859

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Citation Number: 28

Abstract

Potent inhibitors of EGF-dependent protein tyrosine kinase (PTK) activity were synthesized in a series of 5-[(2, 5-dihydroxybenzyl) amino] salicylates. Several of these compounds inhibited EGF-dependent DNA synthesis in ER 22 cells with ICs0< 1 pM. In this series of PTK inhibitors, the role of the salicylate moiety as a potential divalent ion chelator was tested and found to be nonessential in all cases. The length and ramification of the substituting ...