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[Synthesis and biological activity of tyrosine protein kinase inhibitors]
1Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking, Union Medical College, Beijing 100050.
Yao Xue Xue Bao = Acta Pharmaceutica Sinica
|July 1, 1997
Abstract:
Four classes of 25 tyrosine protein kinase (TPK) inhibitors were designed and synthesized. Compounds 1-10 were tested to inhibit TPK of HL-60 leukemia cell using 32P-ATP method, and some of them exhibit evident inhibitory activities. Their structure-activity relationship is similar to that of TPK inhibitors reported in literatures. Compounds 11-25 were tested to inhibit TPK of normal rat spleen cell using ELISA method and their SAR is different from that using 32P-ATP method.