新型C6-哌嗪取代嘌呤甾体核苷类似物的合成及其抗癌活性
Synthesis and anticancer activity of novel C6-piperazine substituted purine steroid-nucleosides analogues.
作者信息
Huang Li-Hua, Xu Hong-De, Yang Zhuo-Ya, Zheng Yong-Fei, Liu Hong-Min
机构信息
College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450001, China; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, China.
School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, China.
出版信息
Steroids. 2014 Apr;82:1-6. doi: 10.1016/j.steroids.2013.12.004. Epub 2013 Dec 28.
Novel C6-piperazine substituted purine nucleoside analogues (2-9) bearing a modified pyranose-like D ring of the 4-azasteroid moiety were efficiently synthesized through nucleophilic substitution at C6 position of the steroid-nucleoside precursors (1) with versatile piperazines. All newly-synthesized compounds were evaluated for their anticancer activity in vitro against Hela, PC-3 and MCF-7 cell lines. Among them, compounds 8b and 9b exhibited significant cytotoxicity on PC-3 cell lines.
通过用多功能哌嗪对甾体 - 核苷前体（1）的C6位进行亲核取代，高效合成了带有修饰的4 - 氮杂甾体部分的吡喃糖样D环的新型C6 - 哌嗪取代嘌呤核苷类似物（2 - 9）。对所有新合成的化合物进行了体外抗Hela、PC - 3和MCF - 7细胞系的抗癌活性评估。其中，化合物8b和9b对PC - 3细胞系表现出显著的细胞毒性。
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