Tyrphostins. 3. Structure-activity relationship studies of. alpha.-substituted benzylidenemalononitrile 5-S-aryltyrphostins

A Gazit, N Osherov, I Posner, A Bar-Sinai…

Index: Gazit, Aviv; Osherov, Nir; Posner, Israel; Bar-Sinai, Allan; Gilon, Chaim; Levitzki, Alexander Journal of Medicinal Chemistry, 1993 , vol. 36, # 23 p. 3556 - 3564

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Citation Number: 42

Abstract

In this study we describe an extension of our previous studies on cis- benzylidenemalononitrile tyrphostins. We have introduced S-aryl substituents in the 5 position (meta vis-a-vis the malononitrile moiety). We find that these compounds are potent blockers of EGFR kinase and its homolog HER-2 kinase. Interestingly, we find that certain S- aryltyrphostins discriminate between EGFR and HER-2 kinase in favor of the HER-2 ...

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