胡国强 杨勇 伊磊 王新 张志强 谢松强 黄文龙. 噁二唑为连接链的C3/C3双氟喹诺酮类化合物的设计、合成与抗肿瘤活性研究(英文)J. 药学学报, 2010,45(8): 1012-1016.
引用本文: 胡国强 杨勇 伊磊 王新 张志强 谢松强 黄文龙. 噁二唑为连接链的C3/C3双氟喹诺酮类化合物的设计、合成与抗肿瘤活性研究(英文)J. 药学学报, 2010,45(8): 1012-1016.
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HU Guo-Jiang, YANG Yong, YI Lei, WANG Xin, ZHANG Zhi-Jiang, XIE Song-Jiang, HUANG Wen-Long. Part II: Design, synthesis and antitumor action of C3/C3 bis- fluoroquinolones linked-cross 2, 5-1, 3, 4oxadiazoleJ. 药学学报, 2010,45(8): 1012-1016.
Citation: HU Guo-Jiang, YANG Yong, YI Lei, WANG Xin, ZHANG Zhi-Jiang, XIE Song-Jiang, HUANG Wen-Long. Part II: Design, synthesis and antitumor action of C3/C3 bis- fluoroquinolones linked-cross 2, 5-1, 3, 4oxadiazoleJ. 药学学报, 2010,45(8): 1012-1016.
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噁二唑为连接链的C3/C3双氟喹诺酮类化合物的设计、合成与抗肿瘤活性研究(英文)

Part II: Design, synthesis and antitumor action of C3/C3 bis- fluoroquinolones linked-cross 2, 5-1, 3, 4oxadiazole

    摘要
  • 摘要:

     以杂环替代抗菌氟喹诺酮的C3位羧基, 以期发现具有抗肿瘤活性的氟喹诺酮小分子探针先导化合物, 选择1, 3, 4-噁二唑杂环作为2分子抗菌氟喹诺酮C3羧基的公共电子等排体, 设计合成了以噁二唑为连接链的C3/C3双氟喹诺酮系列化合物, 其结构通过元素分析和光谱数据得到表征, 评价了体外对L1210、CHO和HL60  3种癌细胞株的生长抑制活性。

     

    Abstract:

    To develop a new small molecular probe for discovering an antitumor lead compound from the replacement of carboxylic group of two molecular antibacterial fluoroquinolones with a heterocyclic ring, a   series of the C3/C3 bis-fluoroquinolones tethered with an 1, 3, 4-oxadiazole ring were synthesized as their    respective HCl salts, and their structures were characterized by elemental analysis and spectral data.  The     in vitro antitumor activity against L1210, CHO and HL60 cell lines was also evaluated via the respective IC50 values by methylthiazole trazolium (MTT) assay.

     

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