In vitro and in vivo pharmacodynamic screening of novel vinflunine derivatives
文献类型：期刊论文
| 作者 | Liu Y(刘悦)2; Lei XS(雷新胜)2; Gong AS(宫爱申)2; Xiao L(肖亮)2; Sun Y(孙易)2; Quan HT(全海天)1 ; Xu YP(徐永平)1; Tang WD(唐卫东)1; Lou LG(楼丽广)1; Deng BC(邓炳初)2
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| 刊名 | Chinese Journal New Drugs
 |
| 出版日期 | 2008 |
| 卷号 | 17期号:19页码:1659 |
| 关键词 | vinfunine anticancer drug screening in vitro |
| ISSN号 | 1003-3734 |
| 其他题名 | 全新长春氟宁衍生物体内外药效筛选 |
| 文献子类 | Article |
| 英文摘要 | Objective:To screen a series of novel vinfunine derivatives in A549 cells in vitro and in human NSCLC A549 nude mice-transplanted tumors in vivo for discovering new candidate compounds with better curative effects and lower toxicities.Methods: Proliferation of A549 cells was measured by the method of SRB as the in vitro pharmacodynamic model.Human NSCLC A549 nude mice-transplanted tumor was used as the in vivo model.Results: The values of IC_(50) of the new derivatives were between 0.05100 mumol·L~(-1) in vitro.As a result,SHR115706 and SHR115766 were chosen as the candidate compounds because their IC_(50) was 0.05 mumol·L~(-1) and 0.29 mumol·L~(-1),respectively.SHR115706 significantly inhibited tumors' growth(P<0.01) in a dose-dependent manner;while SHR115766 obviously inhibited the tumors' growth(P<0.01) in a dose-independent manner.The proliferation rates of tumor cells after treatments with SHR115706(80 mg·kg~(-1)),SHR115766(80 mg·kg~(-1)) and vinfunine(35 mg·kg~(-1),the positive control) were 47.5%,57.6% and 46.5%,respectively.SHR115706 and SHR115766 showed much smaller toxic effects than vinfunine in nude mice.Conclusion: SHR115706 is a superior and promising anticancer compound. |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:3429922 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/268050]  |
| 专题 | 药理学第一研究室 |
| 作者单位 | 1.中国科学院上海生命科学院上海药物研究所, 上海 201203, 中国. 2.上海恒瑞医药有限公司, 上海 200245, 中国.; |
| 推荐引用方式 GB/T 7714 | Liu Y,Lei XS,Gong AS,et al. In vitro and in vivo pharmacodynamic screening of novel vinflunine derivatives[J]. Chinese Journal New Drugs,2008,17(19):1659. |
| APA | 刘悦.,雷新胜.,宫爱申.,肖亮.,孙易.,...&邓炳初.(2008).In vitro and in vivo pharmacodynamic screening of novel vinflunine derivatives.Chinese Journal New Drugs,17(19),1659. |
| MLA | 刘悦,et al."In vitro and in vivo pharmacodynamic screening of novel vinflunine derivatives".Chinese Journal New Drugs 17.19(2008):1659. |
入库方式： OAI收割
来源：上海药物研究所
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