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作者：杨玉社 嵇汝运 陈凯先 丁健
抗肿瘤喹诺酮|左旋氧氟沙星|合成|抗肿瘤活性|抗菌活性
作者：杨玉社 嵇汝运 陈凯先 丁健
单位：中国科学院上海药物研究所，上海 200031
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
药学学报990209 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。
STUDIES ON SYNTHESIS ANTIBACTERIAL AND ANTITUMOR ACTIVITY
OF (S)-(-)-OFLOXACIN ANALOGUES
Yang Yushe(Yang YS), Ji Ruyun(Ji RY), Chen Kaixian(Chen KX) and Ding Jian(Ding J)
(Shanghai Institute of Materia Medica, Shanghai 200031)
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. ......
单位：中国科学院上海药物研究所，上海 200031
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
药学学报990209 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。
STUDIES ON SYNTHESIS ANTIBACTERIAL AND ANTITUMOR ACTIVITY
OF (S)-(-)-OFLOXACIN ANALOGUES
Yang Yushe(Yang YS), Ji Ruyun(Ji RY), Chen Kaixian(Chen KX) and Ding Jian(Ding J)
(Shanghai Institute of Materia Medica, Shanghai 200031)
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. ......