Fluorocyclopentenyl-cytosine with Broad Spectrum and Potent Antitumor Activity
Fluorocyclopentenyl-cytosine with Broad Spectrum and Potent Antitumor Activity
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DOI：
10.1021/jm3004009
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发表时间：
2012-05-10
影响因子：
7.3
通讯作者：
Jeong, Lak Shin
中科院分区：
文献类型：
--
作者：
Choi, Won Jun;Chung, Hwa-Jin;Jeong, Lak Shin
基于环戊烯基嘧啶类化合物的生物活性，以D-核糖为原料，设计合成了含氟环戊烯基嘧啶类化合物。其中，胞嘧啶衍生物5a在广泛的肿瘤细胞系中显示出高度有效的抗生长效果，并且在植入A549人肺癌细胞的裸鼠肿瘤异种移植模型中显示出非常有效的抗肿瘤活性。然而，其2 '-脱氧胞苷衍生物5 b没有显示任何抗生长作用，表明2'-羟基对于生物活性是必需的。
On the basis of the potent biological activity of cyclopentenyl-pyrimidines, fluorocyclopentenyl-pyrimidines were designed and synthesized from D-ribose. Among these, the cytosine derivative 5a showed highly potent antigrowth effects in a broad range of tumor cell lines and very potent antitumor activity in a nude mouse tumor xenograft model implanted with A549 human lung cancer cells. However, its 2'-deoxycytidine derivative 5b did not show any antigrowth effects, indicating that 2'-hydroxyl group is essential for the biological activity.