Four tetrandrine (TET) derivatives (IVa-IVd) have been synthesized by Suzuki reaction of boronic acid derivatives and 5-bromo-tetrandrine obtained by bromination using tetrandrine as the starting material. The structures are analyzed by ¹H NMR, ¹³C NMR and ESI-MS. The inhibition activities of IVa-IVd against HL60 and A549 cancer cell lines have been investigated by CCK-8 assay. The compounds having significant (P <0.040) inhibition activities are secondarily screened by MTT assay. The inhibitory activities of IVa-IVd against protein tyrosine kinases (PTKs) are tested by ELISA. The results show that IVa, IVb and IVc exhibit significant inhibition activities against the two cancer cell lines. The IVb and IVc show highly significant (P <0.001) inhibition activities against fibroblast growth factor receptor 1 (FGFR1).

中文翻译：

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粉防己碱衍生物IVa-IVd：结构分析及其对蛋白酪氨酸激酶，HL60和A549癌细胞系的抑制率

通过硼酸衍生物的铃木反应和以粉防己碱为原料通过溴化得到的5-溴-粉防己碱已经合成了四种粉防己碱（TET）衍生物（IVa-IVd）。通过¹ H NMR，¹³ C NMR和ESI-MS分析结构。通过CCK-8试验研究了IVa-IVd对HL60和A549癌细胞的抑制活性。然后通过MTT测定法筛选具有显着（P＜0.040）抑制活性的化合物。通过ELISA测试IVa-IVd对蛋白酪氨酸激酶（PTK）的抑制活性。结果表明，IVa，IVb和IVc对两种癌细胞系表现出显着的抑制活性。IVb和IVc显示出高度显着性（P <0.001）对成纤维细胞生长因子受体1（FGFR1）的抑制活性。