[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.
Guo
Z R
ZR
Institute of Materia Medica, CAMS, Beijing.
Goto
S
S
Yang
G Z
GZ
Terada
H
H
D001597:Benzylidene Compounds / Q000737:chemistry* / Q000494:pharmacology; D009570:Nitriles / Q000737:chemistry* / Q000494:pharmacology; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013329:Structure-Activity Relationship
D001597:Benzylidene Compounds; D009570:Nitriles; D011505:Protein-Tyrosine Kinases