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学科主题: 天然产物有机化学
题名: A Novel Water-Soluble Gossypol Derivative Increases Chemotherapeutic Sensitivity and Promotes Growth Inhibition in Colon Cancer
其他题名: A Novel Water-Soluble Gossypol Derivative Increases Chemotherapeutic Sensitivity and Promotes Growth Inhibition in Colon Cancer
作者: Yan F(阎飞) ; Cao XX(曹星欣) ; Jiang HX(姜海霞) ; Zhao XL(赵小龙) ; Wang JY(王建永) ; Lin YH(林毅晖) ; Liu QL(刘巧玲) ; Zhang C(张琛) ; Jiang B(姜标) ; Guo F(郭方)
通讯作者: 姜标 ; 郭方
刊名: J. Med. Chem.
发表日期: 2010
卷: 53, 期:15, 页:5502-5510
收录类别: SCI
部门归属: 中国科学院上海生命科学研究院健康科学研究所; 中国科学院上海高等研究院; 中国科学院上海有机化学研究所
英文摘要: Compound 1 ((-)-gossypol) has been long known as a chemical anticancer agent. With its low water solubility and toxicity, it is not widely used as a commercial drug. To overcome these disadvantages, several novel derivatives of gossypol were designed, synthesized, and analyzed. One of the derivatives, compound 7 (6-aminopenicillanic acid sodium-gossypolone), was identified with great water solubility and anticancer property, suggested by inducing a dramatically decrease in Bcl-2 and Bcl-xL protein expression level found in vitro and growth inhibition of murine colon tumor in vivo. Furthermore, it was also recognized with less toxicity than compound 1 in vivo and significantly increased chemotherapeutic sensitivity against colon cancer in combination with traditional chemotherapeutic agent 5-fluorouracil. Therefore, it is concluded that compound 7 is superior to parent compound 1, and further preclinical studies of compound 7 is necessary for colon cancer therapy.
语种: 英语
相关网址: 查看原文
WOS记录号: WOS:000280523300010
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/20279
Appears in Collections:中科院天然产物有机化学重点实验室_期刊论文

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Recommended Citation:
Yan F,Cao XX,Jiang HX,et al. A Novel Water-Soluble Gossypol Derivative Increases Chemotherapeutic Sensitivity and Promotes Growth Inhibition in Colon Cancer[J]. J. Med. Chem.,2010,53(15):5502-5510.
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