目的 合成SU11274衍生物并对其进行受体PTK抑制活性评价.方法 合成了用乙二胺、1,3-丙二胺、1,2-丙二胺、1,6-己二胺替代SU11274哌嗪基团的4个SU11274新衍生物,结构经1H-NMR和ESI-MS验证.采用ELISA方法对这4个化合物进行了受体PTK抑制活性评价.结果 合成的4个SU11274衍生物(5a,5b,5c,5d)均为新化合物.生物学评价结果显示化合物5b的受体PTK抑制活性要显著优于SU11274,化合物5c有非常显著的受体PTK抑制活性,而5a和5d则较弱.结论 SU11274的哌嗪基团被不同二胺取代会影响化合物的受体PTK抑制活性.%Objective To synthesize and evaluate the inhibition of SUl1274 analogs on the receptor tyrosine kinase. Methods Four new SUI 1274 analogs with 1,2-diaminoethane, 1,3-diaminopropane, 1,2-diaminopropane and 1,6-diaminohexane substituting the SUl1274 piperazine group were synthesized. Their structur es were verified by 1H-NMR and ESI-MS. The receptor tyrosine kinase inhibitiory activity was studied by ELISA assay. Results Four SU11274 analogs were new compounds. Biochemicalevaluations demonstrate that receptor tyrosine kinase inhibitory activity of 5 b was significantly better than that of SU 11274, but that of compound 5 c was the most significant. The inhibitory activities of 5 a and 5 b was very low. Conclusion Substitution of the piperazine of SU 11274 with different side chains affects the inhibitory activity of receptor tyrosine kinase of SU11274 analogs.
展开▼
