新型嘌呤-8-酮衍生物的合成及抗肿瘤活性研究
收稿日期: 2016-11-23
修回日期: 2017-01-03
网络出版日期: 2017-02-08
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
Received date: 2016-11-23
Revised date: 2017-01-03
Online published: 2017-02-08
Supported by
Project supported by the National Natural Science Foundation of China (No. 21672127).
张自鹏 , 杨新颖 , 方浩 . 新型嘌呤-8-酮衍生物的合成及抗肿瘤活性研究[J]. 有机化学, 2017 , 37(6) : 1479 -1486 . DOI: 10.6023/cjoc201611031
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
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