Synthesis and pharmacological effects of 3-methyl tyrphostin (2-cyano- 3-[4-hydroxyphenyl]-2-butenethioamide): A new protein tyrosine kinase inhibitor

Centella, C; De La Pena A.M.; Medina, J; Sapag-Hagar, M; Meléndez J.; Lavandero S.; Ocaranza M.P.; Escobedo, J

Keywords: inhibition, enzyme, mouse, phosphorylation, synthesis, protein, proliferation, cell, structure, screening, tyrosine, strain, inhibitor, drug, article, kinase, animal, 3, priority, nonhuman, journal, effect, unclassified, methyltyrphostin, thioamide, 3t3


A novel tyrphostin (2-cyano-3-[4-hydroxyphenyl]-2-butenethioamide) (CHB) with a methyl group adjacent to the aromatic ring has been synthesized. The new compound inhibits the autophosphorylation of the platelet-derived growth factor receptor kinase and the phosphorylation of phosphatidylinositol 3- kinase by this receptor kinase with an IC 50 of approximately 1 ?M. It also decreased the proliferation of a cell line transformed with the keratinocyte growth factor kinase but had no effect on the parent NIH/3T3 cells. Neither cyclic adenosine monophosphate-dependent protein kinase nor protein kinase C activities were affected by the new tyrphostin.

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Título de la Revista: Am J Therapeuthics
Volumen: 3
Número: 6
Fecha de publicación: 1996
Página de inicio: 423
Página final: 426