SYNTHESIS OF NOVEL BIOLOGICALLY ACTIVE NATURAL PRODUCTS

新型生物活性天然产物的合成

• 批准号: 3278052
• 负责人: ROBERT K BOECKMAN
• 金额: $ 9.73万
• 依托单位: UNIVERSITY OF ROCHESTER
• 依托单位国家: 美国
• 财政年份: 1982
• 资助国家: 美国
• 起止时间: 1982-09-15 至 1990-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3278052
• 关键词: antineoplastics; chemical structure function; cycloalkene; drug design /synthesis /production; sesquiterpenes

The objectives are to develop general protocols for the synthesis of three different classes of naturally occurring compounds, Eremantholide A, Saudin, and Ginkgolide A, each of which possesses interesting biological activity and which constitute a lead in a different therapeutic area, namely cancer, diabetes, and cardiovascular disease, asthma and stroke, respectively. The syntheses have been planned with the idea that simpler analog structures will become available during our studies to assist in the development of structure activity relationships in these unique classes of compounds. Our studies will explore new strategies and new applications and methods for creation of contiguous quaternary centers, closure of medium rings, and the construction of hetero propellane systems. The problems posed by these densely functionalized cage and bridged ring structures present considerable challenges for contemporary synthetic organic chemistry.

目标是开发用于合成三种 不同种类的天然存在的化合物，Eremanthropy A， Saudin和Ginkgolide A，它们中的每一种都具有有趣的生物活性， 活性，并在不同的治疗领域构成领先地位， 即癌症、糖尿病、心血管疾病、哮喘和中风， 分别 合成计划的想法是， 在我们的研究期间将提供结构来协助 在这些独特的类的结构活性关系的发展 化合物. 我们的研究将探索新的策略和新的应用和方法 用于产生连续的四元中心，闭合中环，以及 异质螺旋桨系统的构造。 这些问题带来的 存在密集官能化的笼和桥环结构 这是当代有机合成化学面临的巨大挑战。