SYNTHESIS AND ANTITUMOR ACTIVITY OF TERPENOIDS

萜类化合物的合成及其抗肿瘤活性

• 批准号: 3290096
• 负责人: DUY H HUA
• 金额: $ 6.35万
• 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/3290096
• 关键词: antineoplastics; 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.

拟议的研究可以分为三类。 这些都是： (a) 区域选择性、可逆性和机制的研究 手性亚磺酰烯丙基阴离子与环境的不对称加成反应 亲电子试剂、烯酮和烯亚胺，(b) 上述物质的合成应用 反应如不对称全合成所示 (+)-并五烯烯、(+)-并五烯内酯、脱氧并五烯基葡萄糖醛酸和 杂环化合物和(c)紫杉素、紫杉宁和(c)的全合成 紫杉醇通过新型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。 提议的合成是 一般而言，因此可以实现许多类似物。 每个模拟将是 使用体外组织培养系统测试抗肿瘤活性。 一次 活性化合物被鉴定后，将在动物体内进行测试 模型。