新型C6-环仲胺取代嘌呤甾体核苷类似物的合成与生物学评价
Synthesis and biological evaluation of novel C6-cyclo secondary amine substituted purine steroid-nucleosides analogues.
作者信息
Huang Li-Hua, Li Yang, Xu Hong-De, 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.
College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450001, China.
出版信息
Steroids. 2014 Jul;85:13-7. doi: 10.1016/j.steroids.2014.03.017. Epub 2014 Apr 12.
Novel C6-cyclo secondary amine substituted purine steroid-nucleoside analogues (2-9) were efficiently synthesized through displacement of the C6 chloro on the purine ring of series 1 with versatile cyclic secondary amines, including pyrrolidines, piperidine, morpholine, and piperazines. All the newly-synthesized compounds were evaluated for their anticancer activity in vitro against Hela, PC-3 and MCF-7 cell lines. Among them, compounds 5c and 6b exhibited significant cytotoxicity on PC-3 cell lines.
通过用包括吡咯烷、哌啶、吗啉和哌嗪在内的多种环状仲胺取代系列1嘌呤环上的C6氯，高效合成了新型C6-环仲胺取代的嘌呤甾体-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5c和6b对PC-3细胞系表现出显著的细胞毒性。
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