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Synthesis and Cytotoxic Evaluation of Steroidal Copper (Cu (II)) Complexes.
Bioinorganic Chemistry and Applications ( IF 4.7 ) Pub Date : 2017-10-18 , DOI: 10.1155/2017/4276919
Yanmin Huang 1 , Erbin Kong 1 , Junyan Zhan 1 , Shuang Chen 1 , Chunfang Gan 1 , Zhiping Liu 1 , Liping Pang 1 , Jianguo Cui 1, 2
Affiliation  

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 IC50 values of complexes 5 and 12 against Bel-7404 (human liver carcinoma) are 5.0 and 7.0 μM.

中文翻译:

甾族铜(Cu(II))配合物的合成和细胞毒性评价。

以雌酮和孕烯醇酮为起始原料,通过类固醇酮与硫代氨基脲或二氮杂吡啶的缩合反应,然后使甾族硫代氨基脲或甾族二氮杂吡啶与铜(II)的络合反应,合成了一些甾族铜络合物。通过IR,NMR和HRMS表征复合物。筛选合成的化合物对HeLa,Bel-7404和293T细胞系的细胞毒性。结果表明,所有甾体铜(II)配合物均对被测癌细胞具有明显的抗增殖活性。针对Bel-7404(人类肝癌)的复合物512的IC 50值为5.0和 7.0μM .
更新日期:2017-10-18
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