紫檀芪和肉桂酸拼合物的制备及体外抗癌活性研究

来源 :2015年全国药物化学学术会议暨第五届中英药物化学学术会议 | 被引量 : 0次 | 上传用户:fronj
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
其他文献
Berberine has been extensively used to treat intestinal infections,particularly bacterial diarrhea for thousands of years in China.
Nitrogen heteroarenes widely present in naturally occurring products and synthetic bioactive molecules,and as core structures of currently marketed drugs[1].
A series of novel 3-(2,4-dihydroxyphenyl)-propionic acid amides were synthesized and evaluated as tyrosinase inhibitors using a tyrosinase-dependent tyrosine oxidation assay.
Azole ethanol fragment was revealed to be highly beneficial for antimicrobial potency.
Azole rings are an important class of unusual poly-nitrogen aromatic heterocycles able to readily interact with various biological cations,anions,small molecules and macromolecules such as DNAs,enzyme
A series of novel diosmetin derivatives was designed and synthesized using rational drug-design principles.
A series of novel 3,4-dihydroquinoxalin-2(1H)-one derivatives were designed and synthesized via rational drug design.
研究表明,源于原人参二醇的C24 差向异构ocotillol 型人参皂苷的心肌保护作用和ADME 存在显著立体差异[1]。有关其半合成的研究已有报道,但其形成机理的研究报道较少。
以20(S)-原人参二醇和为20(S)-原人参三醇原料,经乙酰化、m-CPBA 氧化和氢氧化钠皂化三步反应,合成得到两对ocotillol 型C24 差向异构体1、2 以及3、4,用1H NMR、13CNMR、HMBC、NOESY 及MS 确证其结构,并通过X-ray 单晶衍射确证差向异构体的立体结构[1]。
前期,我们以20(S)-PPT 为原料,设计经乙酰化、m-CPBA 氧化和皂化反应,得到近乎等物质量的ocotillol(3)及其C24 差向异构体(4)。经X-ray 单晶衍射证实,3 的C24 为R 构型,4 的C24 为S 构型[1]。