Tyrphostins. 6. Dimeric benzylidenemalononitrile tyrphostins: Potent inhibitors of EGF receptor tyrosine kinase in vitro

Aviv Gazit, Nir Osherov, Chaim Gilon, Alexander Levitzki

Research output: Contribution to journalArticlepeer-review

Abstract

Benzylidenemalononitrile (BMN) tyrphostins were previously found to be potent inhibitors of EGF receptor (EGFR) tyrosine kinase activity. Since these compounds were found to compete for the substrate and sometimes with the ATP site and since EGFR acts as a dimer, we prepared a series of dimeric tyrphostins. These dimeric tyrphostins were built from two BMN units linked by various spacers and designed to fit the dimeric cross-autophosphorylation signal transduction intermediate of the EGFR tyrosine kinases. Structure- activity relationship of these potent dimeric EGF receptor tyrosine kinase inhibitors is reported.

Original languageEnglish
Pages (from-to)4905-4911
Number of pages7
JournalJournal of Medicinal Chemistry
Volume39
Issue number25
DOIs
StatePublished - 6 Dec 1996
Externally publishedYes

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