| 含三氮唑基团的新型PI3K抗肿瘤抑制剂的设计与合成 |
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| 引用本文： | 陈绍俊,方渡,樊后兴.含三氮唑基团的新型PI3K抗肿瘤抑制剂的设计与合成[J].化工时刊,2010,24(5):15-19,77. |
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| 作者姓名： | 陈绍俊 方渡 樊后兴 |
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| 作者单位： | 1. 湖南中医药大学,湖南,长沙,410208
2. 上海阳帆医药科技有限公司,上海,201203 |
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| 摘 要： | 以PI3K/Akt信号通路为靶标的小分子抑制剂的研究已成为抗肿瘤新药研究的热点。以GDC-0941为先导物,合成一系列含三氮唑基团的新型PI3K抗肿瘤抑制剂,并进行了体外抗肿瘤活性评价,期望从中筛选出活性优于GDC-0941的新型抗肿瘤候选药物。
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| 关 键 词： | PI3K 合成 含三氮唑基团抑制剂 抗肿瘤活性 |
Design and Synthesis of a Novel Series of Triazole-based PI3-kinase Inhibitors for the Treatment of Cancer |
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| Chen Shaojun,Fang Du,Fan Houxing.Design and Synthesis of a Novel Series of Triazole-based PI3-kinase Inhibitors for the Treatment of Cancer[J].Chemical Industry Times,2010,24(5):15-19,77. |
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| Authors: | Chen Shaojun Fang Du Fan Houxing |
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| Affiliation: | Chen Shaojun Fang Du Fan Houxing (Hunan University of Chinese Medicine,Hunan Changsha 410208; Shanghai Sun-sail Pharmaceutical Science ＆ Technology Co.,Ltd.,Shanghai 201203) |
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| Abstract: | The research of small molecule inhibitors targeting at PI3K/Akt singling pathway has become a hot spot for exploration of new anti-tumor drugs.GDC-0941 selected as a leading compound,a novel series of triazole-based PI3K inhibitors were synthesized and evaluated for their anti-proliferative activities in vitro to find novel candidates with more potent activity than GDC-0941. |
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| Keywords: | PI3K |
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