[The lead generation of protein tyrosine kinase inhibitors by quantitative structure-activity relationship analysis]

Analysis of the quantitative relationship between a series of substituted benzylidenemalononitriles and the inhibitory action on protein tyrosine kinases were carried out using the Hansch-Fujita method. The results indicate that the presence of two or three hydroxy groups attached to a phenyl ring, which connects an extended (trans form) conjugated chain, is essential to the inhibition. Compared with the structure of other kinds of inhibitors, a presumable basic structure for inhibiting the enzyme was generated.