Study on Anti-Proliferative Activity in Cancer Cells and Preliminary Structure-Activity Relationship of Pseudo-Peptide Chiral Thioureas
Study on Anti-Proliferative Activity in Cancer Cells and Preliminary Structure-Activity Relationship of Pseudo-Peptide Chiral Thioureas
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伪肽手性硫脲抗癌细胞增殖活性及初步构效关系研究
DOI：
10.1002/bkcs.11383
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发表时间：
2018
影响因子：
1.7
通讯作者：
Li Yong Jun
中科院分区：
文献类型：
--
作者：
Liao Peng;Hu Shi Qin;Zhang Hong;Xu Liang Bi;Liu Jing Zi;He Bin;Liao Shang Gao;Li Yong Jun
在我们以前的研究中，我们已经表明，含磷酸酯的硫脲类化合物具有强大的抗肿瘤活性，可以作为一种新的策略，用于开发抗肿瘤药物。本文合成了一系列新型的膦酸硫脲类化合物5 - 38，并通过1H NMR、13 C NMR、元素分析等手段对其结构进行了表征。已使用三种人类癌细胞系（Bcap-37、BGC-823和PC-3）来研究这些化合物的抗肿瘤活性。通过构效关系的研究，发现该类化合物中R、R1和R2的变化与抗肿瘤活性有关。所有这些SAR引导的努力可能会在不久的将来在市场上产生新的抗肿瘤药物。
In our previous studies, we have shown that thiourea compounds containing phosphate esters have potent antitumor activity and can be used as a novel strategy for the development of antitumor agents. Herein, a series of novel phosphonate thioureas5–38have been synthesized, which were fully characterized by1H NMR,13C NMR spectrum, elemental analysis. Three human cancer cell lines (Bcap‐37, BGC‐823, and PC‐3) have been used to investigate these compounds’ antitumor activities. After the summarization of the structure–activity relationships, we found that the variation of R, R1, and R2in these novel phosphonate thioureas contribute to the antitumor activities. All these SAR‐guided efforts may lead to novel antitumor drugs in the market in the near future.