Molecular modelling and biological evaluation of a series of hydroxylated benzylideneanilines and benzylamines designed as tyrosine kinase inhibitors.

A series of hydroxylated benzylideneanilines and benzylamines were prepared and tested for inhibition of epidermal growth factor receptor-associated protein tyrosine kinase (PTK) activity in vitro. Molecular modelling and analysis of the biological results lead us to propose a minimal structural pharmacophore for two distinct binding sites within the PTK domain.