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Synthesis and Molecular Recognition of Biologically Active Marine Natural Products

生物活性海洋天然产物的合成与分子识别

基本信息

批准号：
03453037
负责人：
YAMAMURA Shosuke
金额：
$ 4.22万
依托单位：
KEIO UNIVERSITY
依托单位国家：
日本
项目类别：
Grant-in-Aid for General Scientific Research (B)
财政年份：
1991
资助国家：
日本
起止时间：
1991 至 1993
项目状态：
已结题

项目摘要

Recently, a number of interesiting marine natural products with novel structures and biological functions have been found, usually in very small quantities. Accordingly, our great efforts have been focused on total syntheses of these compounds in gram scale, as follows.1)Synthetic studies on pyrroloquinoline alkaloidsA new class of pyrroloquinoline alkaloids have been isolated as metabolites of the New Zealand, Okinawan and Fijian sponges. They show remarkable antitumor activities and particularly possess potent inhibitory activities against the function of topoisomerase II.We successfully synthesized discorhabdin C, batzelline C, isobatzelline C, makaluvamines A, B, C and D.Some of their synthetic intermediates were also proved to have antitumor activities.2)Synthetic studies on novel pyrone-metabolites of some marine organismsPeroniatriols and ilikonapyrone are considered to be defensive substances of some kinds of marine molluscs. We developed new systhetic methodology to construct … More a fully substituted gamma-pyrone ring, and determined the absolute configurations of these pyrones by means of the above mentioned method.3)Synthetic studies on bryostatinsBryostatins, the highly oxygenated macrolides are one of the most attractive marine natural products for their therapeutically antineoplastic activities. Our considerable efforts have been made for syntheses of bryostatin 11 in gram scale. And we could synthesize two main moieties which include all of carbon atoms of bryostatin 11. Further synthetic study on this macrolide is in progress.4)Synthetic studies on bioactive substances produced by marine sponges and sea hearsWe had already synthesized bastadins, aerothionin and related marine natural products, all of which have an interesting spiroisoxazol ring and show antibacterial activities. We further attempt to synthesize psammaplysin which has been isolated as the metabolite of sea hare. We also developed a new synthetic method to construct trans-hydroazulenes, using electrochemical technique, from which a number of marine natural products will be derived. Less

近年来，人们发现了许多有趣的海洋天然产物，它们具有新颖的结构和生物学功能，但通常数量很少。因此，我们的努力集中在以克为单位的这些化合物的全合成上，如下所示。吡咯喹啉类生物碱的合成研究从新西兰、冲绳和斐济海绵的代谢产物中分离出一类新的吡咯喹啉类生物碱。它们具有显著的抗肿瘤活性，特别是对拓扑异构酶II的功能具有较强的抑制作用。我们成功地合成了discorhabdin C， batzelline C, isobabzelline C, makaluvamines A， B， C和d .一些合成的中间体也被证明具有抗肿瘤活性。2)一些海洋生物新型吡咯酮代谢产物的合成研究。吡咯烷醇和吡咯烷酮被认为是一些海洋软体动物的防御物质。我们开发了一种新的合成方法，构建了更多的全取代-吡咯环，并通过上述方法确定了这些吡咯环的绝对构型。苔藓虫素是一种高氧大环内酯类化合物，具有良好的抗肿瘤活性，是近年来备受关注的海洋天然产物之一。我们为合成苔藓虫素11进行了大量的研究工作。我们可以合成包含苔藓抑素11所有碳原子的两个主要部分。该大环内酯的进一步合成研究正在进行中。4)海洋海绵和海hears生物活性物质的合成研究我们已经合成了basadins， aerothionin和相关的海洋天然产物，它们都有一个有趣的螺异唑环，并具有抗菌活性。我们进一步尝试合成已从海兔的代谢产物中分离出来的沙曼菌素。我们还开发了一种新的合成方法，利用电化学技术构建反式氢偶氮烯，从中可以衍生出许多海洋天然产物。少