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.

目标是制定合成三个化合物的通用方案 不同种类的天然化合物，Eremantholide A， 和银杏内酯A，每一种都具有有趣的生物学特性 并在不同的治疗区域中构成铅， 即癌症、糖尿病、心血管疾病、哮喘和中风， 分别进行了分析。 合成的计划是基于这样一个想法，即更简单的模拟 我们将在研究期间提供结构，以帮助 在这些独特的类别中结构活性关系的发展 化合物。 我们的研究将探索新的战略和新的应用和方法 用于创建连续的第四级中心、中环的闭合以及 杂化螺旋桨系统的构建。这些问题带来的问题 存在密集功能化的笼形和桥式环状结构 当代合成有机化学面临相当大的挑战。