Huang Yanmin, Kong Erbin, Zhan Junyan, Chen Shuang, Gan Chunfang, Liu Zhiping, Pang Liping, Cui Jianguo
Key Laboratory of Beibu Gulf Environment Change and Resources Utilization, College of Chemistry and Material Science, Guangxi Teachers Education University, Nanning 530001, China.
Guangxi Colleges and University Key Laboratory of Beibu Gulf Oil and Natural Gas Resource Effective Utilization, Qizhou University, Qizhou, China.
Bioinorg Chem Appl. 2017;2017:4276919. doi: 10.1155/2017/4276919. Epub 2017 Oct 18.
Using estrone and pregnenolone as starting materials, some steroidal copper complexes were synthesized by the condensation of steroidal ketones with thiosemicarbazide or diazanyl pyridine and then complexation of steroidal thiosemicarbazones or steroidal diazanyl pyridines with Cu (II). The complexes were characterized by IR, NMR, and HRMS. The synthesized compounds were screened for their cytotoxicity against HeLa, Bel-7404, and 293T cell lines in vitro. The results show that all steroidal copper (II) complexes display obvious antiproliferative activity against the tested cancer cells. The IC values of complexes and against Bel-7404 (human liver carcinoma) are 5.0 and 7.0 M.
以雌酮和孕烯醇酮为起始原料，通过甾体酮与氨基硫脲或吡啶二氮烯缩合，然后甾体氨基硫脲或甾体吡啶二氮烯与Cu（II）络合，合成了一些甾体铜配合物。通过红外光谱、核磁共振和高分辨质谱对配合物进行了表征。对合成的化合物进行了体外对HeLa、Bel-7404和293T细胞系的细胞毒性筛选。结果表明，所有甾体铜（II）配合物对受试癌细胞均表现出明显的抗增殖活性。配合物 和 对Bel-7404（人肝癌）的IC值分别为5.0和7.0 μM。
