检索结果-南通市图书馆

检索条件"主题词=Anti-tumor drug candidate"

共 1 条记录，以下是1-10 订阅

全选清除本页清除全部题录导出标记到"检索档案"

详细简洁

排序：

Plinabulin:A Marine drug candidate for anti-tumor

Plinabulin:A Marine Drug Candidate for Anti-tumor

引用

第十二届海洋药物学术年会

作者： SUN Tian-wen WANG Shi-xiao ZHAO Jian-chun DING Zhong-peng CHENG He-juan LIU Xiao-chun LIU Li CAI Bing GUAN Hua-shi LI Wen-bao School of Medicine and Pharmacy Ocean University of China Marine Biomedical Research Institute of Qingdao

Plinabulin is a synthesized diketopiperazine type tubulin inhibitor discovered based on the structure-activity relationship（SAR）study of Phenylahistin,which was isolated from *** was observed that Plinabulin binds between alpha and beta tubulin subunit which is close to colchicine-binding site of *** study indicated that it has good efficacy,pharmacokinetics and safety properties,current it is in phaseⅢclinical ***,we are working on optimization of its synthesis *** ethyl isocyanoacetate and three methyl acetic anhydride as starting materials,the imidazole aldehyde was obtained through four steps;and then the target molecule was accomplished through two steps of condensation reaction,the total synthesis yield is 12%.The double bond Z,E isomers can be produced in the second condensation reaction,and the Z isomer,which has anti-tumor activity,can be obtained by avoiding *** screening indicated that Plinabulin has strong inhibition the growth of A431 human skin cancer cell,the inhibition rate was91.8%in 12.5 nm concentration *** intracellular fluorescence intensity of the microtubule protein enhanced,and the cell morphology altered were observed with using Alexa488 *** order to obtain a new generation of anti-tumor drugs with better biological activity and to overcome the existing drug resistance,our group has designed and synthesized a series of novel derivatives based on the structure of ***-001,a new marine anti-tumor drug candidate having good druggability,was selected to preclinical study through activity screening,preliminary pharmacokinetics and safety studies.

关键词： Plinabulin Tubulin inhibitor Marine drug anti-tumor drug candidate

来源： cnki会议评论

在线全文

cnki会议

学校读者我要写书评

暂无评论

全选清除本页清除全部题录导出标记到“检索档案”

共1页 << < 1 > >>

回到顶部

执行限定条件

欢迎您,

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

在线全文

请选择保存的检索档案：

请选择收藏分类：

通借通还

欢迎您,

建议与咨询 留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

在线全文

请选择保存的检索档案： 新增检索档案 确定 取消

请选择收藏分类： 新增自定义分类 确定 取消

通借通还

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

请选择保存的检索档案：

请选择收藏分类：