NATURAL PRODUCT SYNTHESIS VIA EPISULFONIUM ION INITIATED

通过环磺离子引发的天然产物合成

• 批准号: 3292084
• 负责人: THOMAS Stuart LIVINGHOUSE
• 金额: $ 6.56万
• 依托单位: MONTANA STATE UNIVERSITY - BOZEMAN
• 依托单位国家: 美国
• 财政年份: 1987
• 资助国家: 美国
• 起止时间: 1987-09-01 至 1989-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3292084
• 关键词: analgesics; antineoplastics; drug design /synthesis /production; morphinans; polyenes

The objectives will be to develop improved chemical syntheses for biologically significant natural products and their structural analogs. These syntheses are destined to rely upon new procedures for effecting episulfonium ion initiated carboannulations which we have recently discovered. Specific molecules targeted for synthesis include the anti-cancer agent taxodione and the morphinan analgesics. The cytotoxin taxodione has exhibited significant activity in vivo against Walker intramuscular carcinsarcoma 256 in rats and in vitro against cells derived from human carcinoma of the nasopharnyx (KB). The analgesic morphine and its analogs have a rich history of clinical use for the relief of severe pain resulting from physical trauma and chronic illnesses. In addition to the above objectives, the utilization of sulfenium ion promoted cyclizations involving vinylcyclopropane and higher order polyene initiators will be synthetically evaluated.

目标是开发改进的化学合成 生物学意义的天然产物及其结构类似物。 这些综合注定要依靠新程序来实现 发起的发起了我们最近有的碳水化合物 发现。 靶向合成的特定分子包括 抗癌剂Taxodione和吗啡镇痛药。 细胞毒素型taxodione在体内表现出显着的活性 沃克肌内癌症256大鼠和体外针对细胞 源自鼻摩尼克（KB）的人类癌。 镇痛吗啡及其类似物具有丰富的临床使用史 为了缓解因身体创伤和慢性而导致的严重疼痛 疾病。 除了上述目标外，磺基离子的利用 促进涉及乙烯基环丙烷和高阶多烯的环旋 发起人将进行合成评估。