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有机化学
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有机化学 ›› 2017, Vol. 37 ›› Issue (6): 1479-1486.DOI: 10.6023/cjoc201611031 上一篇    下一篇

研究论文

新型嘌呤-8-酮衍生物的合成及抗肿瘤活性研究

张自鹏, 杨新颖, 方浩   

  1. 山东大学药学院 济南 250012
  • 收稿日期:2016-11-23 修回日期:2017-01-03 发布日期:2017-02-08
  • 通讯作者: 方浩 E-mail:haofangcn@sdu.edu.cn
  • 基金资助:

    国家自然科学基金面上（No.21672127）资助项目.

Synthesis and Antiproliferative Activity of Novel Purin-8-one Derivatives

Zhang Zipeng, Yang Xinying, Fang Hao   

  1. School of Pharmaceutical Sciences, Shandong University, Ji'nan 250012
  • Received:2016-11-23 Revised:2017-01-03 Published:2017-02-08
  • Contact: 10.6023/cjoc201611031 E-mail:haofangcn@sdu.edu.cn
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 21672127).

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以2，4-二氯-5-硝基嘧啶为起始原料，通过多步反应制备了一系列新型嘌呤-8-酮衍生物，并经1H NMR、13C NMR和HRMS结构确认.采用四甲基偶氮唑盐（MTT）法测定了目标化合物的体外抗肿瘤细胞增殖活性，结果表明：部分目标化合物具有较好的抗肿瘤细胞增殖活性，其中四个化合物抑制人子宫颈癌细胞（Hela）、人急性淋巴母细胞白血病细胞（MOLT-4）和白血病细胞（K562）的活性相当或优于阳性对照药R-Roscovitine.

关键词: 嘌呤衍生物, 抗肿瘤, 合成

A series of novel purin-8-one derivatives were prepared with the starting materials of 2,4-dichloro-5-nitropyrimidine and followed by multi-step reactions. The structures of all target compounds were identified by 1H NMR, 13C NMR and HRMS. The preliminary biological evaluations were performed using thiazolyl blue tetrazolium bromide (MTT) method to test their antiproliferative activities against some tumor cell lines. The results suggested that some compounds exhibited good anti-proliferative activities against tumor cell lines. Especially, four compounds showed similar or better inhibitory activities against Hela, MOLT-4 and K562 tumor cell lines compared with R-roscovitine.

Key words: purine derivatives, antitumor, synthesis