酪氨酸蛋白激酶抑制剂的合成及生物活性

SYNTHESIS AND BIOLOGICAL ACTIVITY OF TYROSINE PROTEIN KINASE INHIBITORS

设计并合成了四类共２５个酪氨酸蛋白激酶（ＴＰＫ）抑制剂。用ＡＴＰ参入法测定了化合物１～１０对ＨＬ６０白血病来源的ＴＰＫ的抑制作用，有些化合物表现出明显的抑制活性。构效关系（ＳＡＲ）表明，呈现抑制活性的必要结构或基团与文献报道的构效关系相一致。还尝试了酶联免疫吸附法（ＥＬＩＳＡ）测定化合物１１～２５对正常鼠脾来源的ＴＰＫ的抑制作用。

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 32 P 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 32 P ATP method.