| 左旋氧氟沙星类似物的合成及其抗菌抗肿瘤活性研究 |
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| 引用本文： | 杨玉社,嵇汝运,陈凯先,丁健. 左旋氧氟沙星类似物的合成及其抗菌抗肿瘤活性研究[J]. 药学学报, 1999, 34(2): 119-124 |
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| 作者姓名： | 杨玉社 嵇汝运 陈凯先 丁健 |
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| 作者单位： | 中国科学院上海药物研究所,上海,200031 |
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| 基金项目： | 国家自然科学基金,上海市科技启明星计划资助项目 |
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| 摘 要： | 目的：设计合成有抗菌抗肿瘤活性的喹诺酮药物。方法和结果：根据推理药物设计原理，设计并合成了16个新型抗菌抗肿瘤喹诺酮类化合物，并研究其构效关系。结论：用9株细菌及4株肿瘤细胞评价了它们的体外抗菌活性(MIC值)及抗肿瘤活性(抑瘤率%)。其中，化合物16～20有较好的抗肿瘤及抗菌活性。
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| 关 键 词： | 抗肿瘤喹诺酮 左旋氧氟沙星 合成 抗肿瘤活性 抗菌活性 |
| 收稿时间： | 1998-03-30 |
| 修稿时间： | 1998-03-30 |
STUDIES ON SYNTHESIS ANTIBACTERIAL AND ANTITUMOR ACTIVITY OF (S)-(-)-OFLOXACIN ANALOGUES |
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| Yang Yushe,Ji Ruyun,Chen Kaixian,Ding Jian. STUDIES ON SYNTHESIS ANTIBACTERIAL AND ANTITUMOR ACTIVITY OF (S)-(-)-OFLOXACIN ANALOGUES[J]. Acta pharmaceutica Sinica, 1999, 34(2): 119-124 |
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| Authors: | Yang Yushe Ji Ruyun Chen Kaixian Ding Jian |
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| Abstract: | AIM: To design and prepare quinolone compounds with antibacterial and antitumor activities. METHODS AND RESULTS: According to rational drug design principle, a series of novel analogues of (S)-(-)-ofloxacin has been prepared and the influences on structure-activity relationships was also discussed. CONCLUSION: Their in vitro antitumor and antibacterial activities were evaluated. The results showed that compound 16～20 have good antitumor and antibacterial activities. |
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| Keywords: | antitumor quinolone (S) (-) ofloxacin synthesis antitumor activity antibacterial activity |
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