THE LEAD GENERATION OF PROTEIN TYROSINE KINASE INHIBITORS BY QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP ANALYSIS

ZR Guo; S Goto; GZ Yang; H Terada

ZR Guo, S Goto, GZ Yang, H Terada. THE LEAD GENERATION OF PROTEIN TYROSINE KINASE INHIBITORS BY QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP ANALYSISJ. Acta Pharmaceutica Sinica, 1992, 27(2): 90-95.

Citation:

ZR Guo, S Goto, GZ Yang, H Terada. THE LEAD GENERATION OF PROTEIN TYROSINE KINASE INHIBITORS BY QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP ANALYSISJ. Acta Pharmaceutica Sinica, 1992, 27(2): 90-95.

Citation:

ZR Guo, S Goto, GZ Yang, H Terada. THE LEAD GENERATION OF PROTEIN TYROSINE KINASE INHIBITORS BY QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP ANALYSISJ. Acta Pharmaceutica Sinica, 1992, 27(2): 90-95.

THE LEAD GENERATION OF PROTEIN TYROSINE KINASE INHIBITORS BY QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP ANALYSIS

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Abstract

Analysis of the quantitative relationship between a series of substitutedbenzylidenemalononitriles and the inhibitory action on protein tyrosine Kinases were car-ried out using the Hansch- Fujita method. The results indicate that the presence of two orthree 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 kindsof inhibitors, a presumable basic structure for inhibiting the enzyme was generated.

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THE LEAD GENERATION OF PROTEIN TYROSINE KINASE INHIBITORS BY QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP ANALYSIS

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