SYNTHESIS AND BIOLOGICAL ACTIVITY OF TYROSINE PROTEIN KINASE INHIBITORS

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.