植物内生真菌生物碱活性成分的研究进展

大量的生物碱从植物内生真菌中分离了出来, 并表现出良好的生物活性. 对植物内生真菌所产生的生物碱, 按照酰胺类、有机胺类、吡咯类、喹啉和异喹啉类、吲哚类、吡啶类、喹唑啉类进行了综述, 并且介绍了这些生物碱的生物活性.     

苯并啡啶类生物碱及其衍生物合成研究进展

苯并啡啶类生物碱是一类广泛分布于罂粟科和芸香科植物中的天然含氮化合物,具有显著的抗肿瘤和广谱抗菌等多种生物活性.基于苯并啡啶类生物碱的生源合成途径的特殊性对天然苯并啡啶类生物碱结构类型进行了分类.综述了自1999年以来天然苯并啡啶类生物碱及其衍生物的合成方法研究进展,对各个合成路线的特点进行了讨论.     

4-羟基-2-吡啶酮类天然生物碱的研究进展

4-羟基-2-吡啶酮类生物碱是从植物和昆虫等内生真菌发酵液中提取分离得到的一类新型天然生物碱, 具有抗真菌、抗菌和抗肿瘤等多种生物活性. 对近年来4-羟基-2-吡啶酮类天然生物碱的分离、结构确证和全合成等进行了总结和概述, 重点介绍了Ilicilolin H, Tenellin和Sambutaxin等的全合成.     

Saframycins 及Ecteinascidins化合物的合成研究进展

综述了两类双四氢异喹啉生物碱Saframycins和Ecteinascidins的合成研究进展. 分析了各合成路线的关键步骤, 部分讨论了各方法的优缺点, 并对其生物合成和作用机理作了简单介绍.     

加兰他敏类生物碱的不对称合成研究进展

加兰他敏类生物碱是氢化二苯并呋喃类生物碱的重要组成部分.它们独特的结构、良好的生物活性和前景广阔的药用价值吸引了众多化学家和药物学家的兴趣.其合成难点是其中的含芳基手性全碳季碳的构筑.本综述旨在阐述到目前为止加兰他敏类生物碱的不对称合成方法,根据合成路线中手性季碳的构筑方式分类进行说明,并尝试对每种合成方法进行评述.     

Spirotryprostatin类生物碱的合成研究进展

Spirotryprostatin类生物碱是一类具有螺环吲哚二酮哌嗪结构的生物碱,其结构特点是吲哚部分和二酮哌嗪部分通过一个螺碳原子手性中心相连.由于具有这样特殊的结构使得螺环吲哚二酮哌嗪化合物具有一些生理和药理活性,尤其对细胞周期有较好的抑制活性.近年来,spirotryprostatin类生物碱的合成得到了广泛的研究,根据其结构中螺环手性中心形成的方法不同,对spirotryprostatin类生物碱的全合成研究进展进行综述.     

吲哚类生物碱的合成研究进展

吲哚类生物碱是具有吲哚分子骨架的一类化合物,具有多种良好的生理活性。文章综述了近年来新发现吲哚类生物碱的合成研究进展,介绍了(-)-Arboricine,(±)-cis-Trikentrin A,(-)-Corynantheidol等化合物的合成方法。     

景洪哥纳香生物碱的MS-MS 及GC-MS研究

蕃荔枝科哥纳香属植物常作为药用植物使用,可以治疗水肿、风湿病等.哥纳香属植物中生物碱部分包括了阿卟菲类生物碱,1-aza-anthrquinone类生物碱等.本文在利用质谱的不同方法对单体化合物进行裂解特征的研究基础上,采用GC-MS研究了生物总碱中的化学成分.     

抗肿瘤Lamellarin类生物碱的合成研究新进展

Lamellarin类化合物是从海洋软体动物中分离得到的一类生物碱. Lamellarin类生物碱及其类似物具有良好的抑制肿瘤细胞增殖、逆转p-糖蛋白介导的多药耐药等活性, 显示出成为抗肿瘤候选药物的潜力. 近年来, 对Lamellarin类生物碱结构改造和新型杂合体及类似物的研究, 已成为新型抗肿瘤候选药物研究的热点之一. 综述了Lamellarin类生物碱的全合成策略与技术等方面的研究新进展.     

乌头类双酯型生物碱组分转化为单酯水解型及脂型生物碱组分的研究

建立了乌头类双酯型生物碱组分专一的转化为单酯水解型生物碱组分和脂型生物碱组分的方法,其转化率在90%以上,应用电喷雾多级串联质谱方法监测反应进程并对反应产物进行鉴定,同时可以考察反应中生成的副产物.     

Enantioselective syntheses of the alkaloids cis-195A (pumiliotoxin C) and trans-195A based on multiple applications of asymmetric catalysis

Short enantio- and diastereoselective syntheses of the decahydroquinoline alkaloids cis- (pumiliotoxin C) and trans-195A are presented. Key steps are an enantioselective iridium-catalyzed allylic amination, a Suzuki-Miyaura coupling, a catalyst-controlled copper-catalyzed 1,4-addition, and a reductive amination.     

Unified total syntheses of fawcettimine class alkaloids: fawcettimine, fawcettidine, lycoflexine, and lycoposerramine B

The total syntheses of the lycopodium alkaloids fawcettimine, fawcettidine, lycoflexine, and lycoposerramine B have been accomplished through an efficient, unified, and stereocontrolled strategy that relies on a Diels-Alder reaction to construct the cis-fused 6,5-carbocycles with one all-carbon quaternary center. Access to the enantioselective syntheses of both antipodes of those alkaloids can be achieved by kinetic resolution of the earliest intermediate via a Sharpless asymmetric dihydroxylation (Sharpless AD). Compared to existing approaches to these alkaloids, our synthetic route possesses superior stereocontrol over the C-4 and C-15 stereogenic centers as well as allowing for more functional variation on the 6-membered ring.     

Development of new synthetic methods and its application to total synthesis of nitrogen-containing bioactive natural products

A group of naturally occurring substances containing nitrogen is widely distributed in plants as well as in fungi, animal, marine organisms, and insects, and many exhibit significant biological activity. These natural products with a huge variety of chemical structures include antibiotics, antitumor agents, immunostimulants, drugs affecting the cardiovascular and central nervous systems, analgesics etc. The diverse activities and low natural abundance of this group of natural products when coupled with their molecular complexity warrant development of new and efficient synthetic methods and strategy for the total synthesis of these products, in particular alkaloids. The purpose of this review is to describe some of our achievements in the total synthesis of the naturally-occurring bases including the Dendrobatid alkaloids pumiliotoxin B and allopumiliotoxin A, the anitibiotic streptazolin, the tricyclic marine alkaloids isolated from the ascidians such as fasicularin, lepadiformine, and cylindricine C, and the dimeric monoterpene alkaloid incarvillateine as well as the formal total synthesis of the spirocyclic marine alkaloids halichlorine and pinnaic acid, which are isolated from the Japanese marine sponge and the Okinawan bivalve, respectively.     

The absolute configuration of the side chain diol moiety of the poison-frog alkaloid pumiliotoxin B

The absolute configuration of the diol moiety in the side chain of pumiliotoxin B has been established by comparison of the ozonolysis product from pumiliotoxin B diacetate with the synthetic 3,4-diacetoxy-2-pentanone derived from L-(+)-tartaric acid. This indicates the absolute configuration (R, R) of C-15, C-16 diol of pumiliotoxin B.     

Simple indole alkaloids and those with a nonrearranged monoterpenoid unit

This review covers the literature on simple indole alkaloids and those with a nonrearranged monoterpenoid unit. Newly isolated alkaloids, structure determinations, total syntheses and biological activities are included.     

Simple indole alkaloids and those with a nonrearranged monoterpenoid unit

This review covers simple indole alkaloids, isoprenoid tryptamines, and bisindole alkaloids with a nonrearranged monoterpenoid unit. Newly isolated alkaloids, structure determinations, total syntheses and biological activities are reported. The literature from January to December 2000 is reviewed, and 182 references are cited.     

The synthesis of alkaloids of the ergotoxin group. 70. Section on ergot alkaloids

The syntheses of the alkaloids of the ergotoxine-group i.e. ergocristine, α- and β-ergokryptine, and ergocornine, are described. Using starting material with known stereochemistry these syntheses allowed to determine the absolute configurations also at C-2′ and C-12′ in the peptide part, which could not be derived from analytical data. All ergot alkaloids of the peptide type possess the same stereochemical structure.     

Thirty-five years of synthetic studies directed towards the histrionicotoxin family of alkaloids

This article brings together for the first time reviews of all the synthetic attempts towards the spirocyclic histrionicotoxin alkaloids published since the discovery of the group in 1971. This covers 5 total syntheses of the fully unsaturated parent alkaloid HTX-283A, 7 total syntheses of perhydrohistrionicotoxin, 15 total syntheses of other members of this alkaloid family, 25 formal syntheses, and 19 partial syntheses involving the successful formation of the core azaspirocyclic structure but lacking advancement towards the target structure.     

First asymmetric total syntheses of (-)-subincanadines a and B, skeletally rearranged pentacyclic monoterpenoid indole alkaloids in aspidospermasubincanum

We achieved the first asymmetric total syntheses of novel Aspidosperma indole alkaloids, (-)-subincanadines A and B, which involve an intramolecular diastereoselective Pictet-Spengler cyclization and an intramolecular Nozaki-Hiyama-Kishi reaction as key steps in the total syntheses.     

Synthesis of antiproliferative Cephalotaxus esters and their evaluation against several human hematopoietic and solid tumor cell lines: uncovering differential susceptibilities to multidrug resistance

Deoxyharringtonine (2), homoharringtonine (3), homodeoxyharringtonine (4), and anhydroharringtonine (5) are reported to be among the most potent members of the antileukemia alkaloids isolated from the Cephalotaxus genus. Convergent syntheses of these four natural products are described, each involving novel synthetic methods and strategies. These syntheses enabled evaluation of several advanced natural and non-natural compounds against an array of human hematopoietic and solid tumor cells. Potent cytotoxicity was observed in several cell lines previously not challenged with these alkaloids. Variations in the structure of the ester chain within this family of alkaloids confer differing activity profiles against vincristine-resistant HL-60/RV+, signalling new avenues for molecular design of these natural products to combat multi-drug resistance.