SYNTHESIS AND ANTITUMOR ACTIVITY OF TERPENOIDS

萜类化合物的合成及其抗肿瘤活性

• 批准号: 3290091
• 负责人: DUY H HUA
• 金额: $ 5.17万
• 依托单位: KANSAS STATE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1986
• 资助国家: 美国
• 起止时间: 1986-04-04 至 1989-03-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3290091
• 关键词: drug design /synthesis /production; drug screening /evaluation; glucuronates; heterocyclic compounds; lactones; terpenes; tissue /cell culture

The proposed research can be divided into three catagories. These are: (a) studies of the regioselectivity, reversibility and mechanism of the asymmetric addition reaction of chiral sulfinylallyl anions with ambident electrophiles, enones and enimines, (b) synthetic applications of the above reaction as illustrating by the asymmetric total syntheses of (+)-pentalenene, (+)-pentalenolactone, deoxypentalenylglucuron and heterocyclic compounds and (c) total syntheses of taxusin, taxinine and taxol via the novel selective boron-assisted migration reaction of 7-hydroxy-1-methoxybicyclo[2.2.2]-2-octenes. The proposed syntheses are general, thereby a number of analogs can be achieved. Each analog will be tested for antitumor activity using in vitro tissue culture systems. Once the active compounds are identified, they will be tested in vivo animal models.

本文的研究可以分为三大类。 这些是： (a)研究了反应的区域选择性、可逆性和反应机理， 手性亚磺酰基烯丙基阴离子与两亲性试剂的不对称加成反应 亲电试剂、烯酮和烯亚胺，（B）上述化合物的合成应用 不对称全合成反应 （+）-并环戊二烯、（+）-并环戊二烯内酯、脱氧并环戊二烯葡糖醛酸和 杂环化合物和（c）紫杉素、紫杉宁和紫杉醇的全合成。 紫杉醇通过新的选择性硼辅助迁移反应 7-羟基-1-甲氧基双环[2.2.2]-2-辛烯。 建议的合成是 一般来说，由此可以实现许多类似物。 每个模拟将 使用体外组织培养系统测试抗肿瘤活性。 一旦 活性化合物被鉴定，它们将在动物体内进行测试 模型