A new copper(II) complex of dasatinib (DAS) was synthesized and characterized via ESI-MS, UV–Vis, IR, single-crystal X-ray diffraction analysis, ¹H and ¹³C NMR spectroscopy, and elemental analysis. The composition of the new complex (1) was found to be [Cu(DAS + H)(NO₃)₂(H₂O)]NO₃·(H₂O)·(CH₃OH). Through MTT assay, it was found that 1 had high cytotoxicity towards A549, HeLa, BEL-7402, Hep-G2, NCI-H460, and MGC80-3 tumor cell lines, with IC₅₀ values in 4.04–13.04 μM. The Hep-G2 cells were the most sensitive to 1. It is worth noting that compared with DAS and cisplatin, 1 not only had higher in vitro anticancer activity but also exhibited greater selective toxicity towards Hep-G2 cells than for normal HL-7702 cells. Experimental results from cell apoptosis analysis, cellular uptake, TRAP-silver staining assay, RT-PCR, western blot, and transfection assays showed that 1 was most likely a telomerase inhibitor that targeted c-myc G-quadruplex DNA. The high cytotoxicity and biological behaviors of 1 could be correlated with the central copper(II) atom in the coordinated mode with DAS.

合成并通过ESI-MS，UV-Vis，IR，单晶X射线衍射分析，¹ H和¹³ C NMR光谱以及元素分析对达沙替尼（DAS）的新的铜（II）配合物进行了表征。发现新络合物（1）的组成为[Cu（DAS + H）（NO ₃）₂（H ₂ O）] NO ₃ ·（H ₂ O）·（CH ₃ OH）。通过MTT分析，发现1对A549，HeLa，BEL-7402，Hep-G2，NCI-H460和MGC80-3肿瘤细胞系具有高细胞毒性，IC ₅₀值为4.04–13.04μM。Hep-G2细胞对1的敏感性最高。值得注意的是，与DAS和顺铂相比，1不仅具有比常规HL-7702细胞更高的体外抗癌活性，而且还表现出对Hep-G2细胞更大的选择性毒性。细胞凋亡分析，细胞摄取，TRAP-银染色测定，RT-PCR，蛋白质印迹和转染测定的实验结果表明1最有可能是靶向c-myc G-quadruplex DNA的端粒酶抑制剂。高细胞毒性和生物学行为1可以与中央铜（II）与DAS协调模式原子相关。