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天然产物共同药效团导向patriscabratine的抗肿瘤活性
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作者 袁雷 杨元帅 +2 位作者 王志强 王健 孙铁民 《沈阳药科大学学报》 CAS CSCD 北大核心 2012年第11期852-855,共4页
目的基于"天然产物共同药效团"策略探讨天然产物patriscabratine作用靶点,为其深入研究奠定基础。方法通过分子力场分析方法,初步确定与patriscabratine药效结构相似的天然产物aurantiamide acetate为模板分子,鉴于aurantiami... 目的基于"天然产物共同药效团"策略探讨天然产物patriscabratine作用靶点,为其深入研究奠定基础。方法通过分子力场分析方法,初步确定与patriscabratine药效结构相似的天然产物aurantiamide acetate为模板分子,鉴于aurantiamide acetate是通过抑制组织蛋白酶L发挥的抗肿瘤活性,进一步基于组织蛋白酶L的晶体结构,利用分子对接方法,探讨两种天然产物与活性腔的作用模式并进行比对。进一步通过抗肿瘤活性验证计算结果。结果与结论经LigandScout软件分析表明两种天然产物作用方式基本一致,抗肿瘤活性结果表明二者的半数抑制浓度相似。初步确定patriscabratine的作用靶点为组织蛋白酶L。 展开更多
关键词 天然产物共同药效团 patriscabratine aurantiamide ACETATE 分子对接 分子力场 抗肿瘤 活性
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Total synthesis and anticancer activity studies of the stereoisomers of asperphenamate and patriscabratine 被引量:4
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作者 Yuan, Lei Wang, Jin Hui Sun, Tie Min 《Chinese Chemical Letters》 SCIE CAS CSCD 2010年第2期155-158,共4页
All stereoisomers of asperphenamate 1a and patriscabratine 2a were achieved with a high yield,and total synthesis of 2a is firstly described here.The absolute configuration of patriscabratine was determined as(S,S).Th... All stereoisomers of asperphenamate 1a and patriscabratine 2a were achieved with a high yield,and total synthesis of 2a is firstly described here.The absolute configuration of patriscabratine was determined as(S,S).The compounds 1a-d and 2a-d have been tested by MTT assay in T47D,MDA-MB231,HL60,Hela and SGC-7901 cell lines in vitro.Among them,the(R,S) stereoisomer shows the strongest anticancer effects,while the(S,R) shows the weakest one. 展开更多
关键词 N N -substituted phenylalanine-phenylalaninol ester Asperphenamate patriscabratine Total synthesis Anticancer activity
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A New Alkaloid from Patrinia scabra 被引量:5
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作者 Zheng Bing GU Gen Jin YANG +3 位作者 Wen Yong LIU Ting Zhao LI Yan QIU Wei Dong ZHANG 《Chinese Chemical Letters》 SCIE CAS CSCD 2002年第10期957-958,共2页
A new alkaloid has been isolated from the root of Patrinia scabra. Its structure was elucidated as 2'-acetamido-3'-phenyl propyl 2-benzamido-3-phenyl propionate by extensive spectroscopic analysis.
关键词 Patrinia scabra patriscabratine.
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