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目的以L029为先导化合物,设计合成具有蛋白酪氨酸激酶(PTK)抑制活性的化合物。方法以L029为原料,通过还原和(或)在其活泼H等位点接入侧链3-二甲基氨基-1-丙烷、乙酸甲酯、丙酸甲酯等基团,设计合成了一系列L029衍生物,并用酶联免疫吸附法(ELISA)测定其PTK活性,计算抑制率。结果成功合成5个目标化合物,结构经1H NMR和MS确证。其中3个化合物T2、T3、T5具有较强的PTK抑制活性。结论本文研究的目标化合物合成路线方法简单,反应条件温和,3个目标化合物具有较强PTK抑制活性,为进一步开展此类分子的设计合成提供了参考。
Objective To design and synthesize compounds with inhibitory activity of protein tyrosine kinase (PTK) using L029 as the lead compound. Methods L029 was used as a starting material to design and synthesize a series of compounds with side chain 3-dimethylamino-1-propane, methyl acetate and methyl propionate via reduction and / or active H site. Series L029 derivatives, and PTK activity was measured by enzyme-linked immunosorbent assay (ELISA) to calculate the inhibition rate. Results Five target compounds were successfully synthesized and confirmed by 1H NMR and MS. Among them, three compounds T2, T3 and T5 have strong PTK inhibitory activity. Conclusion The target compounds synthesized in this paper are simple and the reaction conditions are mild. The three target compounds have strong PTK inhibitory activity, which provides a reference for further design and synthesis of these molecules.